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  1. Kitamura, S.;  Lin, T.-H.;  Lee, C.-C. D.;  Takamura, A.;  Kadam, R. U.;  Zhang, D.;  Zhu, X.;  Dada, L.;  Nagai, E.;  Yu, W.;  Yao, Y.;  Sharpless, K. B.;  Wilson, I. A.; Wolan, D. W., Ultrapotent Influenza Hemagglutinin Fusion Inhibitors Developed through Sufex-Enabled High-Throughput Medicinal Chemistry. Proc. Natl. Acad. Sci. U. S. A. 2024, 121 (22), e2310677121. https://doi.org/10.1073/pnas.2310677121
  2. Carter, T. R.;  Milosevich, N.;  Dada, L.;  Shaum, J. B.;  Sharpless, K. B.;  Kitamura, S.; Erb, M. A., Sufex-Based Chemical Diversification for the Systematic Discovery of Crbn Molecular Glues. Bioorg. Med. Chem. 2024, 104, 117699. https://doi.org/10.1016/j.bmc.2024.117699
  3. McFadden, W. M.; Casey-Moore, M. C.; Bare, G. A. L.; Kirby, K. A.; Wen, X.; Li, G.; Wang, H.; Slack, R. L.; Snyder, A. A.; Lorson, Z. C.; Kaufman, I. L.; Cilento, M. E.; Tedbury, P. R.; Gembicky, M.; Olson, A. J.; Torbett, B. E.; Sharpless, K. B.; Sarafianos, S. G., Identification of Clickable Hiv-1 Capsid-Targeting Probes for Viral Replication Inhibition. Cell Chem Biol 2024, 31 (3), 477-486.e7. https://doi.org/10.1016/j.chembiol.2024.02.012
  4. Yang, B.; Sukheja, P.; Qin, B.; Li, G.; Bare, G. A. L.; Cascioferro, A.; Love, M. S.; Petrassi, H. M.; Sharpless, K. B.; McNamara, C. W.; Chatterjee, A. K., Synthesis and Structure-Activity Relationships of Aryl Fluorosulfate-Based Inhibitors as Novel Antitubercular Agents. Bioorg. Med. Chem. Lett. 2024, 98, 129596. https://doi.org/10.1016/j.bmcl.2023.129596
  5. Yang, Y.; Chen, M.; Wu, M.; Hong, S.; Gao, B.; Liu, Y.; Yu, C.; Young, T. S.; Chapla, D. G.; Yang, J.-Y.; Cappiello, J. R.; Li, J. P.; Sharpless, K. B.; Moremen, K. W.; Wu, P., Chemoenzymatic Tagging of Tn/Tf/Stf Antigens in Living Systems. Israel Journal of Chemistry 2023, 63 (10-11), e202300081. https://doi.org/10.1002/ijch.202300081
  6. Homer, J. A.; Xu, L.; Kayambu, N.; Zheng, Q.; Choi, E. J.; Kim, B. M.; Sharpless, K. B.; Zuilhof, H.; Dong, J.; Moses, J. E., Sulfur Fluoride Exchange. Nature Reviews Methods Primers 2023, 3 (1), 58. https://doi.org/10.1038/s43586-023-00241-y
  7. Sun, S.; Homer, J. A.; Smedley, C. J.; Cheng, Q.-Q.; Sharpless, K. B.; Moses, J. E., Phosphorus Fluoride Exchange: Multidimensional Catalytic Click Chemistry from Phosphorus Connective Hubs. Chem 2023, 9 (8), 2128-2143. https://doi.org/10.1016/j.chempr.2023.05.013
  8. Xin, Y.; Liu, S.; Liu, Y.; Qian, Z.; Liu, H.; Zhang, B.; Guo, T.; Thompson, G. J.; Stevens, R. C.; Sharpless, K. B.; Dong, J.; Shui, W., Affinity Selection of Double-Click Triazole Libraries for Rapid Discovery of Allosteric Modulators for Glp-1 Receptor. Proc. Natl. Acad. Sci. U. S. A. 2023, 120 (11), e2220767120. https://doi.org/10.1073/pnas.2220767120
  9. Li, H.; Chang, B. S.; Kim, H.; Xie, Z.; Laine, A.; Ma, L.; Xu, T.; Yang, C.; Kwon, J.; Shelton, S. W.; Klivansky, L. M.; Altoe, V.; Gao, B.; Schwartzberg, A. M.; Peng, Z.; Ritchie, R. O.; Xu, T.; Salmeron, M.; Ruiz, R.; Sharpless, K. B.; Wu, P.; Liu, Y., High-Performing Polysulfate Dielectrics for Electrostatic Energy Storage under Harsh Conditions. Joule 2023, 7 (1), 95-111. https://doi.org/10.1016/j.joule.2022.12.010
  10. Cheng, Y.; Li, G.; Smedley, C. J.; Giel, M. C.; Kitamura, S.; Woehl, J. L.; Bianco, G.; Forli, S.; Homer, J. A.; Cappiello, J. R.; Wolan, D. W.; Moses, J. E.; Sharpless, K. B., Diversity Oriented Clicking Delivers Β-Substituted Alkenyl Sulfonyl Fluorides as Covalent Human Neutrophil Elastase Inhibitors. Proc. Natl. Acad. Sci. U. S. A. 2022, 119 (37), e2208540119. https://doi.org/10.1073/pnas.2208540119
  11. Kim, H.; Zhao, J.; Bae, J.; Klivansky, L. M.; Dailing, E. A.; Liu, Y.; Cappiello, J. R.; Sharpless, K. B.; Wu, P., Chain-Growth Sulfur(Vi) Fluoride Exchange Polycondensation: Molecular Weight Control and Synthesis of Degradable Polysulfates. ACS Cent. Sci. 2021, 7 (11), 1919-1928. https://doi.org/10.1021/acscentsci.1c01015
  12. Li, S.; Li, G.; Gao, B.; Pujari, S. P.; Chen, X.; Kim, H.; Zhou, F.; Klivansky, L. M.; Liu, Y.; Driss, H.; Liang, D.-D.; Lu, J.; Wu, P.; Zuilhof, H.; Moses, J.; Sharpless, K. B., Sufexable Polymers with Helical Structures Derived from Thionyl Tetrafluoride. Nature Chemistry 2021, 13 (9), 858-867. https://doi.org/10.1038/s41557-021-00726-x
  13. Sun, S.; Gao, B.; Chen, J.; Sharpless, K. B.; Dong, J., Fluorosulfuryl Isocyanate Enabled Sufex Ligation of Alcohols and Amines. Angewandte Chemie International Edition 2021, 60 (39), 21195-21199. https://doi.org/10.1002/anie.202105583
  14. Zhang, J.; Zhao, X.; Cappiello, J. R.; Yang, Y.; Cheng, Y.; Liu, G.; Fang, W.; Luo, Y.; Zhang, Y.; Dong, J.; Zhang, L.; Sharpless, K. B., Identification of Simple Arylfluorosulfates as Potent Agents against Resistant Bacteria. Proc. Natl. Acad. Sci. U. S. A. 2021, 118 (28), e2103513118. https://doi.org/10.1073/pnas.2103513118
  15. Shyong, Y.-J.; Sepulveda, Y.; Garcia, A.; Samskey, N. M.; Radic, Z.; Sit, R. K.; Sharpless, K. B.; Momper, J. D.; Taylor, P., Enhancing Target Tissue Levels and Diminishing Plasma Clearance of Ionizing Zwitterionic Antidotes in Organophosphate Exposures. Journal of Pharmacology and Experimental Therapeutics 2021, 378 (3), 315-321. https://doi.org/10.1124/jpet.121.000715
  16. Garnar-wortzel, L.; Bishop, T. R.; Kitamura, S.; Milosevich, N.; Asiaban, J. N.; Zhang, X.; Zheng, Q.; Chen, E.; Ramos, A. R.; Ackerman, C. J.; Hampton, E. N.; Chatterjee, A. K.; Young, T. S.; Hull, M. V.; Sharpless, K. B.; Cravatt, B. F.; Wolan, D. W.; Erb, M. A., Chemical Inhibition of Enl/Af9 Yeats Domains in Acute Leukemia. ACS Cent. Sci. 2021, 7 (5), 815-830. https://doi.org/10.1021/acscentsci.0c01550
  17. Taylor, P.; Shyong, Y.-J.; Samskey, N.; Ho, K.-Y.; Radic’, Z.; Fenical, W.; Sharpless, K. B.; Kovarik, Z.; Camacho-Hernandez, G.-A., Ligand Design for Human Acetylcholinesterase and Nicotinic Acetylcholine Receptors, Extending Beyond the Conventional and Canonical. Journal of Neurochemistry 2021, 158 (6), 1217-1222. https://doi.org/10.1111/jnc.15335
  18. Sharpless, K. B., Eric Jacobsen@60, a Personal Statement. Adv. Synth. Catal. 2020, 362 (2), 281-284. https://doi.org/10.1002/adsc.201901658
  19. Zheng, Q.; Xu, H.; Wang, H.; Du, W.-G. H.; Wang, N.; Xiong, H.; Gu, Y.; Noodleman, L.; Sharpless, K. B.; Yang, G.; Wu, P., Sulfur [18f]Fluoride Exchange Click Chemistry Enabled Ultrafast Late-Stage Radiosynthesis. J. Am. Chem. Soc. 2021, 143 (10), 3753-3763. https://doi.org/10.1021/jacs.0c09306
  20. Brighty, G. J.; Botham, R. C.; Li, S.; Nelson, L.; Mortenson, D. E.; Li, G.; Morisseau, C.; Wang, H.; Hammock, B. D.; Sharpless, K. B.; Kelly, J. W., Using Sulfuramidimidoyl Fluorides That Undergo Sulfur(Vi) Fluoride Exchange for Inverse Drug Discovery. Nat. Chem. 2020, 12 (10), 906-913. https://doi.org/10.1038/s41557-020-0530-4
  21. Kitamura, S.; Zheng, Q.; Woehl, J. L.; Solania, A.; Chen, E.; Dillon, N.; Hull, M. V.; Kotaniguchi, M.; Cappiello, J. R.; Kitamura, S.; Nizet, V.; Sharpless, K. B.; Wolan, D. W., Sulfur(Vi) Fluoride Exchange (Sufex)-Enabled High-Throughput Medicinal Chemistry. J. Am. Chem. Soc. 2020, 142 (25), 10899-10904. https://doi.org/10.1021/jacs.9b13652
  22. Lauwaet, T.; Miyamoto, Y.; Iharaid, S.; Le, C.; Kalisiak, J.; Korthals, K. A.; Ghassemian, M.; Smith, D. K.; Sharpless, K. B.; Fokin, V. V.; Eckmann, L., Click Chemistry-Facilitated Comprehensive Identification of Proteins Adducted by Antimicrobial 5-Nitroimidazoles for Discovery of Alternative Drug Targets against Giardiasis. PLoS Neglected Trop. Dis. 2020, 14 (4), e0008224. https://doi.org/10.1371/journal.pntd.0008224
  23. Smedley, C. J.; Li, G.; Barrow, A. S.; Gialelis, T. L.; Giel, M.-C.; Ottonello, A.; Cheng, Y.; Kitamura, S.; Wolan, D. W.; Sharpless, K. B.; Moses, J. E., Diversity Oriented Clicking (Doc): Divergent Synthesis of Sufexable Pharmacophores from 2-Substituted-Alkynyl-1-Sulfonyl Fluoride (Sasf) Hubs. Angew. Chem., Int. Ed. 2020, 59 (30), 12460-12469. https://doi.org/10.1002/anie.202003219
  24. Macek Hrvat, N.; Kalisiak, J.; Sinko, G.; Radic, Z.; Sharpless, K. B.; Taylor, P.; Kovarik, Z., Evaluation of High-Affinity Phenyltetrahydroisoquinoline Aldoximes, Linked through Anti-Triazoles, as Reactivators of Phosphylated Cholinesterases. Toxicol. Lett. 2020, 321, 83-89. https://doi.org/10.1016/j.toxlet.2019.12.016
  25. Meng, G.; Guo, T.; Ma, T.; Zhang, J.; Shen, Y.; Sharpless, K. B.; Dong, J., Modular Click Chemistry Libraries for Functional Screens Using a Diazotizing Reagent. Nature (London, U. K.) 2019, 574 (7776), 86-89. https://doi.org/10.1038/s41586-019-1589-1
  26. Zheng, Q.; Woehl, J. L.; Kitamura, S.; Santos-Martins, D.; Smedley, C. J.; Li, G.; Forli, S.; Moses, J. E.; Wolan, D. W.; Sharpless, K. B., Sufex-Enabled, Agnostic Discovery of Covalent Inhibitors of Human Neutrophil Elastase. Proc. Natl. Acad. Sci. U. S. A. 2019, 116 (38), 18808-18814. https://doi.org/10.1073/pnas.1909972116
  27. Hong, S.; Shi, Y.; Wu, N. C.; Grande, G.; Douthit, L.; Wang, H.; Zhou, W.; Sharpless, K. B.; Wilson, I. A.; Xie, J.; Wu, P., Bacterial Glycosyltransferase-Mediated Cell-Surface Chemoenzymatic Glycan Modification. Nat. Commun. 2019, 10 (1), 1-11. https://doi.org/10.1038/s41467-019-09608-w
  28. Kovarik, Z.; Kalisiak, J.; Hrvat, N. M.; Katalinic, M.; Zorbaz, T.; Zunec, S.; Green, C.; Radic, Z.; Fokin, V. V.; Sharpless, K. B.; Taylor, P., Reversal of Tabun Toxicity Enabled by a Triazole-Annulated Oxime Library-Reactivators of Acetylcholinesterase. Chem. – Eur. J. 2019, 25 (16), 4100-4114. https://doi.org/10.1002/chem.201805051
  29. Kovarik, Z.; Macek Hrvat, N.; Kalisiak, J.; Katalinic, M.; Sit, R. K.; Zorbaz, T.; Radic, Z.; Fokin, V. V.; Sharpless, K. B.; Taylor, P., Counteracting Tabun Inhibition by Reactivation by Pyridinium Aldoximes That Interact with Active Center Gorge Mutants of Acetylcholinesterase. Toxicol. Appl. Pharmacol. 2019, 372, 40-46. https://doi.org/10.1016/j.taap.2019.04.007
  30. Liu, F.; Wang, H.; Li, S.; Bare, G. A. L.; Chen, X.; Wang, C.; Moses, J. E.; Wu, P.; Sharpless, K. B., Biocompatible Sufex Click Chemistry: Thionyl Tetrafluoride (Sof4)-Derived Connective Hubs for Bioconjugation to DNA and Proteins. Angew. Chem., Int. Ed. 2019, 58 (24), 8029-8033. https://doi.org/10.1002/anie.201902489
  31. Taylor, P.; Yan-Jye, S.; Momper, J.; Hou, W.; Camacho-Hernandez, G. A.; Radic, Z.; Rosenberg, Y.; Kovarik, Z.; Sit, R.; Sharpless, K. B., Assessment of Ionizable, Zwitterionic Oximes as Reactivating Antidotal Agents for Organophosphate Exposure. Chem.-Biol. Interact. 2019, 308, 194-197. https://doi.org/10.1016/j.cbi.2019.05.015
  32. Smedley, C. J.; Zheng, Q.; Gao, B.; Li, S.; Molino, A.; Duivenvoorden, H. M.; Parker, B. S.; Wilson, D. J. D.; Sharpless, K. B.; Moses, J. E., Bifluoride Ion Mediated Sufex Trifluoromethylation of Sulfonyl Fluorides and Iminosulfur Oxydifluorides. Angew. Chem., Int. Ed. 2019, 58 (14), 4552-4556. https://doi.org/10.1002/anie.201813761
  33. Sit, R. K.; Kovarik, Z.; Hrvat, N. M.; Zunec, S.; Green, C.; Fokin, V. V.; Sharpless, K. B.; Radic, Z.; Taylor, P., Pharmacology, Pharmacokinetics, and Tissue Disposition of Zwitterionic Hydroxyiminoacetamido Alkylamines as Reactivating Antidotes for Organophosphate Exposure. J. Pharmacol. Exp. Ther. 2018, 367 (2), 363-372. https://doi.org/10.1124/jpet.118.249383
  34. Gahtory, D.; Sen, R.; Pujari, S.; Li, S.; Zheng, Q.; Moses, J. E.; Sharpless, K. B.; Zuilhof, H., Quantitative and Orthogonal Formation and Reactivity of Sufex Platforms. Chem. – Eur. J. 2018, 24 (41), 10550-10556. https://doi.org/10.1002/chem.201802356
  35. Guo, T.; Meng, G.; Zhan, X.; Yang, Q.; Ma, T.; Xu, L.; Sharpless, K. B.; Dong, J., A New Portal to Sufex Click Chemistry: A Stable Fluorosulfuryl Imidazolium Salt Emerging as an “F-So2+” Donor of Unprecedented Reactivity, Selectivity, and Scope. Angew. Chem., Int. Ed. 2018, 57 (10), 2605-2610. https://doi.org/10.1002/anie.201712429
  36. Liu, Z.; Li, J.; Li, S.; Li, G.; Sharpless, K. B.; Wu, P., Sufex Click Chemistry Enabled Late-Stage Drug Functionalization. J. Am. Chem. Soc. 2018, 140 (8), 2919-2925. https://doi.org/10.1021/jacs.7b12788
  37. Gao, B.; Li, S.; Wu, P.; Moses, J. E.; Sharpless, K. B., Sufex Chemistry of Thionyl Tetrafluoride (SOF4) with Organolithium Nucleophiles: Synthesis of Sulfonimidoyl Fluorides, Sulfoximines, Sulfonimidamides, and Sulfonimidates. Angew. Chem., Int. Ed. 2018, 57 (7), 1939-1943. https://doi.org/10.1002/anie.201712145
  38. Mortenson, D. E.; Brighty, G. J.; Plate, L.; Bare, G.; Chen, W.; Li, S.; Wang, H.; Cravatt, B. F.; Forli, S.; Powers, E. T.; Sharpless, K. B.; Wilson, I. A.; Kelly, J. W., “Inverse Drug Discovery” Strategy to Identify Proteins That Are Targeted by Latent Electrophiles as Exemplified by Aryl Fluorosulfates. J. Am. Chem. Soc. 2018, 140 (1), 200-210. https://doi.org/10.1021/jacs.7b08366
  39. Gao, B.; Zhang, L.; Zheng, Q.; Zhou, F.; Klivansky, L. M.; Lu, J.; Liu, Y.; Dong, J.; Wu, P.; Sharpless, K. B., Bifluoride-Catalysed Sulfur(Vi) Fluoride Exchange Reaction for the Synthesis of Polysulfates and Polysulfonates. Nat. Chem. 2017, 9 (11), 1083-1088. https://doi.org/10.1038/nchem.2796
  40. Wang, H.; Zhou, F.; Ren, G.; Zheng, Q.; Chen, H.; Gao, B.; Klivansky, L.; Liu, Y.; Wu, B.; Xu, Q.; Lu, J.; Sharpless, K. B.; Wu, P., Sufex-Based Polysulfonate Formation from Ethenesulfonyl Fluoride-Amine Adducts. Angew. Chem., Int. Ed. 2017, 56 (37), 11203-11208. https://doi.org/10.1002/anie.201701160
  41. Kim, W. J.; Korthals, K. A.; Li, S.; Le, C.; Kalisiak, J.; Sharpless, K. B.; Fokin, V. V.; Miyamoto, Y.; Eckmann, L., Click Chemistry-Facilitated Structural Diversification of Nitrothiazoles, Nitrofurans, and Nitropyrroles Enhances Antimicrobial Activity against Giardia Lamblia. Antimicrob. Agents Chemother. 2017, 61 (6), e02397/1-e02397/12. https://doi.org/10.1128/aac.02397-16
  42. Zha, G.-F.; Zheng, Q.; Leng, J.; Wu, P.; Qin, H.-L.; Sharpless, K. B., Palladium-Catalyzed Fluorosulfonylvinylation of Organic Iodides. Angew. Chem., Int. Ed. 2017, 56 (17), 4849-4852. https://doi.org/10.1002/anie.201701162
  43. Li, S.; Wu, P.; Moses, J. E.; Sharpless, K. B., Multidimensional Sufex Click Chemistry: Sequential Sulfur(Vi) Fluoride Exchange Connections of Diverse Modules Launched from an Sof4 Hub. Angew. Chem., Int. Ed. 2017, 56 (11), 2903-2908. https://doi.org/10.1002/anie.201611048
  44. Silverman, S. M.; Moses, J. E.; Sharpless, K. B., Reengineering Antibiotics to Combat Bacterial Resistance: Click Chemistry [1,2,3]-Triazole Vancomycin Dimers with Potent Activity against Mrsa and Vre. Chem. – Eur. J. 2017, 23 (1), 79-83. https://doi.org/10.1002/chem.201604765
  45. Zheng, Q.; Dong, J.; Sharpless, K. B., Ethenesulfonyl Fluoride (Esf): An on-Water Procedure for the Kilogram-Scale Preparation. J. Org. Chem. 2016, 81 (22), 11360-11362. https://doi.org/10.1021/acs.joc.6b01423
  46. Qin, H.-L.; Zheng, Q.; Bare, G. A. L.; Wu, P.; Sharpless, K. B., A Heck-Matsuda Process for the Synthesis of Β-Arylethenesulfonyl Fluorides: Selectively Addressable Bis-Electrophiles for Sufex Click Chemistry. Angew. Chem., Int. Ed. 2016, 55 (45), 14155-14158. https://doi.org/10.1002/anie.201608807
  47. Chen, W.; Dong, J.; Plate, L.; Mortenson, D. E.; Brighty, G. J.; Li, S.; Liu, Y.; Galmozzi, A.; Lee, P. S.; Hulce, J. J.; Cravatt, B. F.; Saez, E.; Powers, E. T.; Wilson, I. A.; Sharpless, K. B.; Kelly, J. W., Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(S) through Chemoselective Sufex Reaction with a Binding Site Tyr Residue. J. Am. Chem. Soc. 2016, 138 (23), 7353-7364. https://doi.org/10.1021/jacs.6b02960
  48. Zhang, E.; Tang, J.; Li, S.; Wu, P.; Moses, J. E.; Sharpless, K. B., Chemoselective Synthesis of Polysubstituted Pyridines from Heteroaryl Fluorosulfates. Chem. – Eur. J. 2016, 22 (16), 5692-5697. https://doi.org/10.1002/chem.201600167
  49. Bourne, Y.; Sharpless, K. B.; Taylor, P.; Marchot, P., Steric and Dynamic Parameters Influencing in Situ Cycloadditions to Form Triazole Inhibitors with Crystalline Acetylcholinesterase. J. Am. Chem. Soc. 2016, 138 (5), 1611-1621. https://doi.org/10.1021/jacs.5b11384
  50. Toguchi, S.; Hirose, T.; Yorita, K.; Fukui, K.; Sharpless, K. B.; ÅŒmura, S.; Sunazuka, T., in Situ Click Chemistry for the Identification of a Potent D-Amino Acid Oxidase Inhibitor. Chemical and Pharmaceutical Bulletin 2016, 64 (7), 695-703. https://doi.org/10.1248/cpb.c15-00867
  51. Chen, W.; Dong, J.; Li, S.; Liu, Y.; Wang, Y.; Yoon, L.; Wu, P.; Sharpless, K. B.; Kelly, J. W., Synthesis of Sulfotyrosine-Containing Peptides by Incorporating Fluorosulfated Tyrosine Using an Fmoc-Based Solid-Phase Strategy. Angew. Chem., Int. Ed. 2016, 55 (5), 1835-1838. https://doi.org/10.1002/anie.201509016
  52. Baranczak, A.; Liu, Y.; Connelly, S.; Du, W.-G. H.; Greiner, E. R.; Genereux, J. C.; Wiseman, R. L.; Eisele, Y. S.; Bradbury, N. C.; Dong, J.; Noodleman, L.; Sharpless, K. B.; Wilson, I. A.; Encalada, S. E.; Kelly, J. W., A Fluorogenic Aryl Fluorosulfate for Intraorganellar Transthyretin Imaging in Living Cells and in Caenorhabditis Elegans. J. Am. Chem. Soc. 2015, 137 (23), 7404-7414. https://doi.org/10.1021/jacs.5b03042
  53. Liang, Q.; Xing, P.; Huang, Z.; Dong, J.; Sharpless, K. B.; Li, X.; Jiang, B., Palladium-Catalyzed, Ligand-Free Suzuki Reaction in Water Using Aryl Fluorosulfates. Org. Lett. 2015, 17 (8), 1942-1945. https://doi.org/10.1021/acs.orglett.5b00654
  54. Sharpless, K. B.; Finn, M. G.; Martin, V. S., Tsutomu Katsuki (1946-2014). Angew. Chem., Int. Ed. 2015, 54 (16), 4708. https://doi.org/10.1002/anie.201501065
  55. Dong, J.; Krasnova, L.; Finn, M. G.; Sharpless, K. B., Sulfur(Vi) Fluoride Exchange (Sufex): Another Good Reaction for Click Chemistry. Angew. Chem., Int. Ed. 2014, 53 (36), 9430-9448. https://doi.org/10.1002/anie.201309399
  56. Dong, J.; Sharpless, K. B.; Kwisnek, L.; Oakdale, J. S.; Fokin, V. V., Sufex-Based Synthesis of Polysulfates. Angew. Chem., Int. Ed. 2014, 53 (36), 9466-9470. https://doi.org/10.1002/anie.201403758
  57. Sit, R. K.; Fokin, V. V.; Amitai, G.; Sharpless, K. B.; Taylor, P.; Radic, Z., Imidazole Aldoximes Effective in Assisting Butyrylcholinesterase Catalysis of Organophosphate Detoxification. J. Med. Chem. 2014, 57 (4), 1378-1389. https://doi.org/10.1021/jm401650z
  58. Fraser, B. H.; Hamilton, S.; Krause-Heuer, A. M.; Wright, P. J.; Greguric, I.; Tucker, S. P.; Draffan, A. G.; Fokin, V. V.; Sharpless, K. B., Synthesis of 1,4-Triazole Linked Zanamivir Dimers as Highly Potent Inhibitors of Influenza a and B. MedChemComm 2013, 4 (2), 383-386. https://doi.org/10.1039/C2MD20300F
  59. Morris, G. M.; Green, L. G.; Radic, Z.; Taylor, P.; Sharpless, K. B.; Olson, A. J.; Grynszpan, F., Automated Docking with Protein Flexibility in the Design of Femtomolar “Click Chemistry” Inhibitors of Acetylcholinesterase. J. Chem. Inf. Model. 2013, 53 (4), 898-906. https://doi.org/10.1021/ci300545a
  60. Miyamoto, Y.; Kalisiak, J.; Korthals, K.; Lauwaet, T.; Cheung, D. Y.; Lozano, R.; Cobo, E. R.; Upcroft, P.; Upcroft, J. A.; Berg, D. E.; Gillin, F. D.; Fokin, V. V.; Sharpless, K. B.; Eckmann, L., Expanded Therapeutic Potential in Activity Space of Next-Generation 5-Nitroimidazole Antimicrobials with Broad Structural Diversity. Proc. Natl. Acad. Sci. U. S. A. 2013, 110 (43), 17564-17569, S17564/1-S17564/127. https://doi.org/10.1073/pnas.1302664110
  61. Hirose, T.; Maita, N.; Gouda, H.; Koseki, J.; Yamamoto, T.; Sugawara, A.; Nakano, H.; Hirono, S.; Shiomi, K.; Watanabe, T.; Taniguchi, H.; Sharpless, K. B.; Omura, S.; Sunazuka, T., Observation of the Controlled Assembly of Preclick Components in the in Situ Click Chemistry Generation of a Chitinase Inhibitor. Proc. Natl. Acad. Sci. U. S. A. 2013, 110 (40), 15892-15897,S15892/1-S15892/5. https://doi.org/10.1073/pnas.1315049110
  62. Grimster, N. P.; Connelly, S.; Baranczak, A.; Dong, J.; Krasnova, L. B.; Sharpless, K. B.; Powers, E. T.; Wilson, I. A.; Kelly, J. W., Aromatic Sulfonyl Fluorides Covalently Kinetically Stabilize Transthyretin to Prevent Amyloidogenesis While Affording a Fluorescent Conjugate. J. Am. Chem. Soc. 2013, 135 (15), 5656-5668. https://doi.org/10.1021/ja311729d
  63. Yamauchi, J. G.; Gomez, K.; Grimster, N.; Dufouil, M.; Nemecz, A.; Fotsing, J. R.; Ho, K.-Y.; Talley, T. T.; Sharpless, K. B.; Fokin, V. V.; Taylor, P., Synthesis of Selective Agonists for the Α7 Nicotinic Acetylcholine Receptor with in Situ Click-Chemistry on Acetylcholine-Binding Protein Templates. Mol. Pharmacol. 2012, 82 (4), 687-699. https://doi.org/10.1124/mol.112.080291
  64. Radic, Z.; Sit, R. K.; Kovarik, Z.; Berend, S.; Garcia, E.; Zhang, L.; Amitai, G.; Green, C.; Radic, B.; Fokin, V. V.; Sharpless, K. B.; Taylor, P., Refinement of Structural Leads for Centrally Acting Oxime Reactivators of Phosphylated Cholinesterases. J. Biol. Chem. 2012, 287 (15), 11798-11809. https://doi.org/10.1074/jbc.M111.333732
  65. Grimster, N. P.; Stump, B.; Fotsing, J. R.; Weide, T.; Talley, T. T.; Yamauchi, J. G.; Nemecz, A.; Kim, C.; Ho, K.-Y.; Sharpless, K. B.; Taylor, P.; Fokin, V. V., Generation of Candidate Ligands for Nicotinic Acetylcholine Receptors Via in Situ Click Chemistry with a Soluble Acetylcholine Binding Protein Template. J. Am. Chem. Soc. 2012, 134 (15), 6732-6740. https://doi.org/10.1021/ja3001858
  66. Sit, R. K.; Radic, Z.; Gerardi, V.; Zhang, L.-M.; Garcia, E.; Katalinic, M.; Amitai, G.; Kovarik, Z.; Fokin, V. V.; Sharpless, K. B.; Taylor, P., New Structural Scaffolds for Centrally Acting Oxime Reactivators of Phosphylated Cholinesterases. J. Biol. Chem. 2011, 286 (22), 19422-19430. https://doi.org/10.1074/jbc.M111.230656
  67. Millward, S. W.; Henning, R. K.; Kwong, G. A.; Pitram, S.; Agnew, H. D.; Deyle, K. M.; Nag, A.; Hein, J.; Lee, S. S.; Lim, J.; Pfeilsticker, J. A.; Sharpless, K. B.; Heath, J. R., Iterative in Situ Click Chemistry Assembles a Branched Capture Agent and Allosteric Inhibitor for Akt1. J. Am. Chem. Soc. 2011, 133 (45), 18280-18288. https://doi.org/10.1021/ja2064389
  68. Gastaminza, P.; Pitram, S. M.; Dreux, M.; Krasnova, L. B.; Whitten-Bauer, C.; Dong, J.; Chung, J.; Fokin, V. V.; Sharpless, K. B.; Chisari, F. V., Antiviral Stilbene 1,2-Diamines Prevent Initiation of Hepatitis C Virus Rna Replication at the Outset of Infection. J. Virol. 2011, 85 (11), 5513-5523. https://doi.org/10.1128/JVI.02116-10
  69. Cochran, R.; Kalisiak, J.; Kucukkilinc, T.; Radic, Z.; Garcia, E.; Zhang, L.-M.; Ho, K.-Y.; Amitai, G.; Kovarik, Z.; Fokin, V. V.; Sharpless, K. B.; Taylor, P., Oxime-Assisted Acetylcholinesterase Catalytic Scavengers of Organophosphates That Resist Aging. J. Biol. Chem. 2011, 286 (34), 29718-29724, S29718/1-S29718/10. https://doi.org/10.1074/jbc.M111.264739
  70. Weide, T.; Saldanha, S. A.; Minond, D.; Spicer, T. P.; Fotsing, J. R.; Spaargaren, M.; Frere, J.-M.; Bebrone, C.; Sharpless, K. B.; Hodder, P. S.; Fokin, V. V., Nh-1,2,3-Triazole Inhibitors of the Vim-2 Metallo-Β-Lactamase. ACS Med. Chem. Lett. 2010, 1 (4), 150-154. https://doi.org/10.1021/ml900022q
  71. Radic, Z.; Kalisiak, J.; Fokin, V. V.; Sharpless, K. B.; Taylor, P., Interaction Kinetics of Oximes with Native, Phosphylated and Aged Human Acetylcholinesterase. Chem.-Biol. Interact. 2010, 187 (1-3), 163-166. https://doi.org/10.1016/j.cbi.2010.04.014
  72. Vanacore, R.; Ham, A.-J. L.; Voehler, M.; Sanders, C. R.; Conrads, T. P.; Veenstra, T. D.; Sharpless, K. B.; Dawson, P. E.; Hudson, B. G., A Sulfilimine Bond Identified in Collagen Iv. Science (Washington, DC, U. S.) 2009, 325 (5945), 1230-1234. https://doi.org/10.1126/science.1176811
  73. Valdez, C. A.; Tripp, J. C.; Miyamoto, Y.; Kalisiak, J.; Hruz, P.; Andersen, Y. S.; Brown, S. E.; Kangas, K.; Arzu, L. V.; Davids, B. J.; Gillin, F. D.; Upcroft, J. A.; Upcroft, P.; Fokin, V. V.; Smith, D. K.; Sharpless, K. B.; Eckmann, L., Synthesis and Electrochemistry of 2-Ethenyl and 2-Ethanyl Derivatives of 5-Nitroimidazole and Antimicrobial Activity against Giardia Lamblia. J. Med. Chem. 2009, 52 (13), 4038-4053. https://doi.org/10.1021/jm900356n
  74. Minond, D.; Saldanha, S. A.; Subramaniam, P.; Spaargaren, M.; Spicer, T.; Fotsing, J. R.; Weide, T.; Fokin, V. V.; Sharpless, K. B.; Galleni, M.; Bebrone, C.; Lassaux, P.; Hodder, P., Inhibitors of Vim-2 by Screening Pharmacologically Active and Click-Chemistry Compound Libraries. Bioorg. Med. Chem. 2009, 17 (14), 5027-5037. https://doi.org/10.1016/j.bmc.2009.05.070
  75. Kalisiak, J.; Trauger, S. A.; Kalisiak, E.; Morita, H.; Fokin, V. V.; Adams, M. W. W.; Sharpless, K. B.; Siuzdak, G., Identification of a New Endogenous Metabolite and the Characterization of Its Protein Interactions through an Immobilization Approach. J. Am. Chem. Soc. 2009, 131 (1), 378-386. https://doi.org/10.1021/ja808172n
  76. Hirose, T.; Sunazuka, T.; Sugawara, A.; Endo, A.; Iguchi, K.; Yamamoto, T.; Ui, H.; Shiomi, K.; Watanabe, T.; Sharpless, K. B.; Omura, S., Chitinase Inhibitors: Extraction of the Active Framework from Natural Argifin and Use of in Situ Click Chemistry. J. Antibiot. 2009, 62 (5), 277-282. https://doi.org/10.1038/ja.2009.28
  77. Hein, J. E.; Tripp, J. C.; Krasnova, L. B.; Sharpless, K. B.; Fokin, V. V., Copper(I)-Catalyzed Cycloaddition of Organic Azides and 1-Iodoalkynes. Angew. Chem., Int. Ed. 2009, 48 (43), 8018-8021, S8018/1-S8018/64. https://doi.org/10.1002/anie.200903558
  78. Agnew, H. D.; Rohde, R. D.; Millward, S. W.; Nag, A.; Yeo, W.-S.; Hein, J. E.; Pitram, S. M.; Tariq, A. A.; Burns, V. M.; Krom, R. J.; Fokin, V. V.; Sharpless, K. B.; Heath, J. R., Iterative in Situ Click Chemistry Creates Antibody-Like Protein-Capture Agents. Angew. Chem., Int. Ed. 2009, 48 (27), 4944-4948, S4944/1-S4944/29. https://doi.org/10.1002/anie.200900488
  79. V. V. Fokin, V. V. Rostovtsev, L. G. Green, F. Himo and K. B. Sharpless, Copper-Catalysed Ligation of Azides and Acetylenes, U.S. Patent Number 7,375,234, issued May 20, 2008
  80. Yoo, E. J.; Ahlquist, M.; Bae, I.; Sharpless, K. B.; Fokin, V. V.; Chang, S., Mechanistic Studies on the Cu-Catalyzed Three-Component Reactions of Sulfonyl Azides, 1-Alkynes and Amines, Alcohols, or Water: Dichotomy Via a Common Pathway. J. Org. Chem. 2008, 73 (14), 5520-5528. https://doi.org/10.1021/jo800733p
  81. Radic, Z.; Manetsch, R.; Fournier, D.; Sharpless, K. B.; Taylor, P., Probing Gorge Dimensions of Cholinesterases by Freeze-Frame Click Chemistry. Chem.-Biol. Interact. 2008, 175 (1-3), 161-165. https://doi.org/10.1016/j.cbi.2008.04.048
  82. Kwok, S. W.; Hein, J. E.; Fokin, V. V.; Sharpless, K. B., Regioselective Synthesis of Either 1h- or 2h-1,2,3- Triazoles Via Michael Addition to Α,S-Unsaturated Ketones. Heterocycles 2008, 76 (2), 1141-1154. 
  83. Kalisiak, J.; Sharpless, K. B.; Fokin, V. V., Efficient Synthesis of 2-Substituted-1,2,3-Triazoles. Org. Lett. 2008, 10 (15), 3171-3174. https://doi.org/10.1021/ol8006748
  84. Van der Eycken, E.; Sharpless, K. B., Click Chemistry. QSAR Comb. Sci. 2007, 26 (11-12), 1115. https://doi.org/10.1002/qsar.200790024
  85. Sugawara, A.; Sunazuka, T.; Hirose, T.; Nagai, K.; Yamaguchi, Y.; Hanaki, H.; Sharpless, K. B.; Omura, S., Design and Synthesis Via Click Chemistry of 8,9-Anhydroerythromycin a 6,9-Hemiketal Analogues with Anti-Mrsa and -Vre Activity. Bioorg. Med. Chem. Lett. 2007, 17 (22), 6340-6344. https://doi.org/10.1016/j.bmcl.2007.08.068
  86. Finn, M. G.; Kolb, H. C.; Fokin, V. V.; Sharpless, K. B., Concept and Applications of Click Chemistry. From the Standpoint of Advocates. Kagaku to Kogyo (Tokyo, Jpn.) 2007, 60 (10), 976-980.
  87. Vestberg, R.; Malkoch, M.; Kade, M.; Wu, P.; Fokin, V. V.; Sharpless, K. B.; Drockenmuller, E.; Hawker, C. J., Role of Architecture and Molecular Weight in the Formation of Tailor-Made Ultrathin Multilayers Using Dendritic Macromolecules and Click Chemistry. J. Polym. Sci., Part A: Polym. Chem. 2007, 45 (14), 2835-2846. https://doi.org/10.1002/pola.22178
  88. Liu, Y.; Diaz, D. D.; Accurso, A. A.; Sharpless, K. B.; Fokin, V. V.; Finn, M. G., Click Chemistry in Materials Synthesis. Iii. Metal-Adhesive Polymers from Cu(I)-Catalyzed Azide-Alkyne Cycloaddition. J. Polym. Sci., Part A: Polym. Chem. 2007, 45 (22), 5182-5189. https://doi.org/10.1002/pola.22262
  89. Hawker, C. J.; Fokin, V. V.; Finn, M. G.; Sharpless, K. B., Bringing Efficiency to Materials Synthesis: The Philosophy of Click Chemistry. Aust. J. Chem. 2007, 60 (6), 381-383. https://doi.org/10.1071/CH07107
  90. Yoo, E. J.; Ahlquist, M.; Kim, S. H.; Bae, I.; Fokin, V. V.; Sharpless, K. B.; Chang, S., Copper-Catalyzed Synthesis of N-Sulfonyl-1,2,3-Triazoles: Controlling Selectivity. Angew. Chem., Int. Ed. 2007, 46 (10), 1730-1733. https://doi.org/10.1002/anie.200604241
  91. Narayan, S.; Fokin, V. V.; Sharpless, K. B. In Chemistry ‘on Water’ – Organic Synthesis in Aqueous Suspension, Blackwell Publishing Ltd.: 2007; pp 350-365.
  92. Hirose, T.; Sunazuka, T.; Noguchi, Y.; Yamaguchi, Y.; Hanaki, H.; Sharpless, K. B.; Omura, S., Rapid ‘Sar’ Via Click Chemistry: An Alkyne-Bearing Spiramycin Is Fused with Diverse Azides to Yield New Triazole-Antibacterial Candidates. Heterocycles 2006, 69, 55-61.
  93. Sharpless, K. B.; Manetsch, R., In Situ Click Chemistry: A Powerful Means for Lead Discovery. Expert Opin. Drug Discovery 2006, 1 (6), 525-538. https://doi.org/10.1517/17460441.1.6.525
  94. Whiting, M.; Tripp, J. C.; Lin, Y.-C.; Lindstrom, W.; Olson, A. J.; Elder, J. H.; Sharpless, K. B.; Fokin, V. V., Rapid Discovery and Structure-Activity Profiling of Novel Inhibitors of Human Immunodeficiency Virus Type 1 Protease Enabled by the Copper(I)-Catalyzed Synthesis of 1,2,3-Triazoles and Their Further Functionalization. J. Med. Chem. 2006, 49 (26), 7697-7710. https://doi.org/10.1021/jm060754+
  95. Díaz, D. D.; Converso, A.; Sharpless, K. B.; Finn, M. G., 2,6-Dichloro-9-Thiabicyclo[3.3.1]Nonane: Multigram Display of Azide and Cyanide Components on a Versatile Scaffold. Molecules 2006, 11 (4), 212-218. https://doi.org/10.3390/11040212
  96. Whiting, M.; Muldoon, J.; Lin, Y.-C.; Silverman, S. M.; Lindstrom, W.; Olson, A. J.; Kolb, H. C.; Finn, M. G.; Sharpless, K. B.; Elder, J. H.; Fokin, V. V., Inhibitors of Hiv-1 Protease by Using in Situ Click Chemistry. Angew. Chem., Int. Ed. 2006, 45 (9), 1435-1439. https://doi.org/10.1002/anie.200502161
  97. Radic, Z.; Manetsch, R.; Krasinski, A.; Raushel, J.; Yamauchi, J.; Garcia, C.; Kolb, H.; Sharpless, K. B.; Taylor, P., Molecular Basis of Interactions of Cholinesterases with Tight Binding Inhibitors. Chem.-Biol. Interact. 2005, 157-158, 133-141. https://doi.org/10.1016/j.cbi.2005.10.020
  98. Bourne, Y.; Radic, Z.; Kolb, H. C.; Sharpless, K. B.; Taylor, P.; Marchot, P., Structural Insights into Conformational Flexibility at the Peripheral Site and within the Active Center Gorge of Ache. Chem.-Biol. Interact. 2005, 157-158, 159-165. https://doi.org/10.1016/j.cbi.2005.10.018
  99. Wu, P.; Malkoch, M.; Hunt, J. N.; Vestberg, R.; Kaltgrad, E.; Finn, M. G.; Fokin, V. V.; Sharpless, K. B.; Hawker, C. J., Multivalent, Bifunctional Dendrimers Prepared by Click Chemistry. Chem. Commun. (Cambridge, U. K.) 2005, (46), 5775-5777. https://doi.org/10.1039/b512021g
  100. Zhang, L.; Chen, X.; Xue, P.; Sun, H. H. Y.; Williams, I. D.; Sharpless, K. B.; Fokin, V. V.; Jia, G., Ruthenium-Catalyzed Cycloaddition of Alkynes and Organic Azides. J. Am. Chem. Soc. 2005, 127 (46), 15998-15999. https://doi.org/10.1021/ja054114s
  101. Loren, J. C.; Krasinski, A.; Fokin, V. V.; Sharpless, K. B., Nh-1,2,3-Triazoles from Azidomethyl Pivalate and Carbamates: Base-Labile N-Protecting Groups. Synlett 2005, (18), 2847-2850. https://doi.org/10.1055/s-2005-918944
  102. Johnson, S. M.; Petrassi, H. M.; Palaninathan, S. K.; Mohamedmohaideen, N. N.; Purkey, H. E.; Nichols, C.; Chiang, K. P.; Walkup, T.; Sacchettini, J. C.; Sharpless, K. B.; Kelly, J. W., Bisaryloxime Ethers as Potent Inhibitors of Transthyretin Amyloid Fibril Formation. J. Med. Chem. 2005, 48 (5), 1576-1587. https://doi.org/10.1021/jm049274d
  103. Loren, J. C.; Sharpless, K. B., The Banert Cascade: A Synthetic Sequence to Polyfunctional Nh-1,2,3-Triazoles. Synthesis 2005, (9), 1514-1520. https://doi.org/10.1055/s-2005-869892
  104. Feldman, A. K.; Colasson, B.; Sharpless, K. B.; Fokin, V. V., The Allylic Azide Rearrangement: Achieving Selectivity. J. Am. Chem. Soc. 2005, 127 (39), 13444-13445. https://doi.org/10.1021/ja050622q
  105. K. B. Sharpless, M. Andersson, R. Epple and V. V. Fokin, Second Cycle Asymmetric Dihydroxylation Reaction, U.S. Patent Number 6,852,874 B2, issued February 8, 2005.
  106. Krasinski, A.; Radic, Z.; Manetsch, R.; Raushel, J.; Taylor, P.; Sharpless, K. B.; Kolb, H. C., In Situ Selection of Lead Compounds by Click Chemistry: Target-Guided Optimization of Acetylcholinesterase Inhibitors. J. Am. Chem. Soc. 2005, 127 (18), 6686-6692. https://doi.org/10.1021/ja043031t
  107. Narayan, S.; Muldoon, J.; Finn, M. G.; Fokin, V. V.; Kolb, H. C.; Sharpless, K. B., “On Water”: Unique Reactivity of Organic Compounds in Aqueous Suspension. Angew. Chem., Int. Ed. 2005, 44 (21), 3275-3279. https://doi.org/10.1002/anie.200462883
  108. Mocharla, V. P.; Colasson, B.; Lee, L. V.; Roeper, S.; Sharpless, K. B.; Wong, C.-H.; Kolb, H. C., In Situ Click Chemistry: Enzyme-Generated Inhibitors of Carbonic Anhydrase Ii. Angew. Chem., Int. Ed. 2005, 44 (1), 116-120. https://doi.org/10.1002/anie.200461580
  109. Himo, F.; Lovell, T.; Hilgraf, R.; Rostovtsev, V. V.; Noodleman, L.; Sharpless, K. B.; Fokin, V. V., Copper(I)-Catalyzed Synthesis of Azoles. Dft Study Predicts Unprecedented Reactivity and Intermediates. J. Am. Chem. Soc. 2005, 127 (1), 210-216. https://doi.org/10.1021/ja0471525
  110. Chan, T. R.; Hilgraf, R.; Sharpless, K. B.; Fokin, V. V., Polytriazoles as Copper(I)-Stabilizing Ligands in Catalysis. Org. Lett. 2004, 6 (17), 2853-2855. https://doi.org/10.1021/ol0493094
  111. Manetsch, R.; Krasinski, A.; Radic, Z.; Raushel, J.; Taylor, P.; Sharpless, K. B.; Kolb, H. C., In Situ Click Chemistry: Enzyme Inhibitors Made to Their Own Specifications. J. Am. Chem. Soc. 2004, 126 (40), 12809-12818. https://doi.org/10.1021/ja046382g
  112. Converso, A.; Saaidi, P.-L.; Sharpless, K. B.; Finn, M. G., Nucleophilic Substitution by Grignard Reagents on Sulfur Mustards. J. Org. Chem. 2004, 69 (21), 7336-7339. https://doi.org/10.1021/jo0489869
  113. Diaz, D. D.; Punna, S.; Holzer, P.; McPherson, A. K.; Sharpless, K. B.; Fokin, V. V.; Finn, M. G., Click Chemistry in Materials Synthesis. 1. Adhesive Polymers from Copper-Catalyzed Azide-Alkyne Cycloaddition. J. Polym. Sci., Part A: Polym. Chem. 2004, 42 (17), 4392-4403. https://doi.org/10.1002/pola.20330
  114. Wu, P.; Feldman, A. K.; Nugent, A. K.; Hawker, C. J.; Scheel, A.; Voit, B.; Pyun, J.; Frechet, J. M. J.; Sharpless, K. B.; Fokin, V. V., Efficiency and Fidelity in a Click-Chemistry Route to Triazole Dendrimers by the Copper(I)-Catalyzed Ligation of Azides and Alkynes. Angew. Chem., Int. Ed. 2004, 43 (30), 3928-3932. https://doi.org/10.1002/anie.200454078
  115. Krasinski, A.; Fokin, V. V.; Sharpless, K. B., Direct Synthesis of 1,5-Disubstituted-4-Magnesio-1,2,3-Triazoles, Revisited. Org. Lett. 2004, 6 (8), 1237-1240. https://doi.org/10.1021/ol0499203
  116. Bourne, Y.; Kolb, H. C.; Radic, Z.; Sharpless, K. B.; Taylor, P.; Marchot, P., Freeze-Frame Inhibitor Captures Acetylcholinesterase in a Unique Conformation. Proc. Natl. Acad. Sci. U. S. A. 2004, 101 (6), 1449-1454. https://doi.org/10.1073/pnas.0308206100
  117. Kitayama, T.; Yokoi, T.; Kawai, Y.; Hill, R. K.; Morita, M.; Okamoto, T.; Yamamoto, Y.; Fokin, V. V.; Sharpless, K. B.; Sawada, S., The Chemistry of Zerumbone. Part 5: Structural Transformation of the Dimethylamine Derivatives. Tetrahedron 2003, 59 (26), 4857-4866. https://doi.org/10.1016/S0040-4020(03)00667-7
  118. Kolb, H. C.; Sharpless, K. B., The Growing Impact of Click Chemistry on Drug Discovery. Drug Discovery Today 2003, 8 (24), 1128-1137. https://doi.org/10.1016/S1359-6446(03)02933-7
  119. Brik, A.; Muldoon, J.; Lin, Y.-c.; Elder, J. H.; Goodsell, D. S.; Olson, A. J.; Fokin, V. V.; Sharpless, K. B.; Wong, C.-h., Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of Hiv Protease Inhibitors. ChemBioChem 2003, 4 (11), 1246-1248. https://doi.org/10.1002/cbic.200300724
  120. Lee, L. V.; Mitchell, M. L.; Huang, S.-J.; Fokin, V. V.; Sharpless, K. B.; Wong, C.-H., A Potent and Highly Selective Inhibitor of Human Α-1,3-Fucosyltransferase Via Click Chemistry. J. Am. Chem. Soc. 2003, 125 (32), 9588-9589. https://doi.org/10.1021/ja0302836
  121. A. E. Rubin and K. B. Sharpless, Synthesis of α,β–Substituted Amino Amides, Esters, and Acids, U.S. Patent Number 6,573,387, issued June 3, 2003.
  122. Himo, F.; Demko, Z. P.; Noodleman, L.; Sharpless, K. B., Why Is Tetrazole Formation by Addition of Azide to Organic Nitriles Catalyzed by Zinc(Ii) Salts? J. Am. Chem. Soc. 2003, 125 (33), 9983-9987. https://doi.org/10.1021/ja030204q
  123. Ripka, A. S.; Diaz, D. D.; Sharpless, K. B.; Finn, M. G., First Practical Synthesis of Formamidine Ureas and Derivatives. Org. Lett. 2003, 5 (9), 1531-1533. https://doi.org/10.1021/ol034287r
  124. G. Li and K. B. Sharpless, Two Step Synthesis of D–and L–α–Amino Acids and D– and L–α–Amino Aldehydes, U.S. Patent Number 6,509,506, issued January 21, 2003.
  125. Wang, Q.; Chan, T. R.; Hilgraf, R.; Fokin, V. V.; Sharpless, K. B.; Finn, M. G., Bioconjugation by Copper(I)-Catalyzed Azide-Alkyne [3 + 2] Cycloaddition. J. Am. Chem. Soc. 2003, 125 (11), 3192-3193. https://doi.org/10.1021/ja021381e
  126. Himo, F.; Demko, Z. P.; Noodleman, L.; Sharpless, K. B., Mechanisms of Tetrazole Formation by Addition of Azide to Nitriles. J. Am. Chem. Soc. 2002, 124 (41), 12210-12216. https://doi.org/10.1021/ja0206644
  127. Rostovtsev, V. V.; Green, L. G.; Fokin, V. V.; Sharpless, K. B., A Stepwise Huisgen Cycloaddition Process: Copper(I)-Catalyzed Regioselective “Ligation” of Azides and Terminal Alkynes. Angew. Chem., Int. Ed. 2002, 41 (14), 2596-2599. https://doi.org/10.1002/1521-3773(20020715)41:14<2596::AID-ANIE2596>3.0.CO;2-4
  128. Demko, Z. P.; Sharpless, K. B., An Expedient Route to the Tetrazole Analogs of Α-Amino Acids. Org. Lett. 2002, 4 (15), 2525-2527. https://doi.org/10.1021/ol020096x
  129. Sharpless, K. B., Searching for New Reactivity (Nobel Lecture). Angew. Chem., Int. Ed. 2002, 41 (12), 2024-2032. https://doi.org/10.1002/1521-3773(20020617)41:12<2024::AID-ANIE2024>3.0.CO;2-O
  130. V. V. Fokin and K. B. Sharpless, Aminohydroxylation of Olefins, U.S. Patent Number 6,350,905, issued February 26, 2002.
  131. Demko, Z. P.; Sharpless, K. B., A Click Chemistry Approach to Tetrazoles by Huisgen 1,3-Dipolar Cycloaddition: Synthesis of 5-Acyltetrazoles from Azides and Acyl Cyanides. Angew. Chem., Int. Ed. 2002, 41 (12), 2113-2116. https://doi.org/10.1002/1521-3773(20020617)41:12<2113::AID-ANIE2113>3.0.CO;2-Q
  132. Demko, Z. P.; Sharpless, K. B., A Click Chemistry Approach to Tetrazoles by Huisgen 1,3-Dipolar Cycloaddition: Synthesis of 5-Sulfonyl Tetrazoles from Azides and Sulfonyl Cyanides. Angew. Chem., Int. Ed. 2002, 41 (12), 2110-2113. https://doi.org/10.1002/1521-3773(20020617)41:12<2110::AID-ANIE2110>3.0.CO;2-7
  133. Lewis, W. G.; Green, L. G.; Grynszpan, F.; Radic, Z.; Carlier, P. R.; Taylor, P.; Finn, M. G.; Sharpless, K. B., Click Chemistry in Situ: Acetylcholinesterase as a Reaction Vessel for the Selective Assembly of a Femtomolar Inhibitor from an Array of Building Blocks. Angew. Chem., Int. Ed. 2002, 41 (6), 1053-1057. https://doi.org/10.1002/1521-3773(20020315)41:6<1053::AID-ANIE1053>3.0.CO;2-4
  134. Dupau, P.; Epple, R.; Thomas, A. A.; Fokin, V. V.; Sharpless, K. B., Osmium-Catalyzed Dihydroxylation of Olefins in Acidic Media: Old Process, New Tricks. Adv. Synth. Catal. 2002, 344(3+4), 421-433. https://doi.org/10.1002/1615-4169(200206)344:3/4<421::AID-ADSC421>3.0.CO;2-F
  135. Andersson, M. A.; Epple, R.; Fokin, V. V.; Sharpless, K. B., A New Approach to Osmium-Catalyzed Asymmetric Dihydroxylation and Aminohydroxylation of Olefins. Angew. Chem., Int. Ed. 2002, 41 (3), 472-475. https://doi.org/10.1002/1521-3773(20020201)41:3<472::AID-ANIE472>3.0.CO;2-7
  136. Schlingloff, G.; Sharpless, K. B., Asymmetric Aminohydroxylation, in “Asymmetric Oxidation Reactions: A Practical Approach in Chemistry”, T. Katsuki, ed., Oxford University Press: 2001; pp 104-114.
  137. Sharpless, K. B., Searching for New Reactivity. Prix Nobel 2001, 225-241.
  138. Demko, Z. P.; Sharpless, K. B., An Intramolecular [2 + 3] Cycloaddition Route to Fused 5-Heterosubstituted Tetrazoles. Org. Lett. 2001, 3 (25), 4091-4094. https://doi.org/10.1021/ol010220x
  139. Demko, Z. P.; Sharpless, K. B., Preparation of 5-Substituted 1h-Tetrazoles from Nitriles in Water. J. Org. Chem. 2001, 66 (24), 7945-7950. https://doi.org/10.1021/jo010635w
  140. A. K. Yudin and K. B. Sharpless, Epoxidation of Olefins, U.S. Patent number 6,271,400, issued August 7, 2001.
  141. Converso, A.; Burow, K.; Marzinzik, A.; Sharpless, K. B.; Finn, M. G., 2,6-Dichloro-9-Thiabicyclo[3.3.1]Nonane: A Privileged, Bivalent Scaffold for the Display of Nucleophilic Components. J. Org. Chem. 2001, 66 (12), 4386-4392. https://doi.org/10.1021/jo015632y
  142. Fokin, V. V.; Sharpless, K. B., A Practical and Highly Efficient Aminohydroxylation of Unsaturated Carboxylic Acids. Angew. Chem., Int. Ed. 2001, 40 (18), 3455-3457. https://doi.org/10.1002/1521-3773(20010917)40:18<3455::AID-ANIE3455>3.0.CO;2-I
  143. Becker, H.; Sharpless, K. B. In Asymmetric Dihydroxylation, Oxford University Press: 2001; pp 81-104.
  144. Petrassi, H. M.; Sharpless, K. B.; Kelly, J. W., The Copper-Mediated Cross-Coupling of Phenylboronic Acids and N-Hydroxyphthalimide at Room Temperature: Synthesis of Aryloxyamines. Org. Lett. 2001, 3 (1), 139-142. https://doi.org/10.1021/ol0003533
  145. Kolb, H. C.; Finn, M. G.; Sharpless, K. B., Click Chemistry: Diverse Chemical Function from a Few Good Reactions. Angew. Chem., Int. Ed. 2001, 40 (11), 2004-2021. https://doi.org/10.1002/1521-3773(20010601)40:11<2004::AID-ANIE2004>3.0.CO;2-5
  146. Marzinzik, A. L.; Sharpless, K. B., A Simple Method for the Preparation of N-Sulfonylsulfilimines from Sulfides. J. Org. Chem. 2001, 66 (2), 594-596. https://doi.org/10.1021/jo0012039
  147. Chuang, T.-H.; Sharpless, K. B., Applications of Aziridinium Ions. Selective Syntheses of Α,Β-Diamino Esters, Α-Sulfanyl-Β-Amino Esters, Β-Lactams, and 1,5-Benzodiazepin-2-One. Org. Lett. 2000, 2 (23), 3555-3557. https://doi.org/10.1021/ol000221+
  148. Chuang, T.-H.; Sharpless, K. B., Applications of Aziridinium Ions: Selective Syntheses of Pyrazolidin-3-Ones and Pyrazolo[1,2-a]Pyrazoles. Helv. Chim. Acta 2000, 83 (8), 1734-1743. https://doi.org/10.1002/1522-2675(20000809)83:8<1734::AID-HLCA1734>3.0.CO;2-E
  149. B. Tao, G. Schlingloff and K. B. Sharpless, Synthesis of Aryl Serines, U.S. Patent number 6,057,473, issued May 2, 2000.
  150. Demko, Z. P.; Bartsch, M.; Sharpless, K. B., Primary Amides. A General Nitrogen Source for Catalytic Asymmetric Aminohydroxylation of Olefins. Org. Lett. 2000, 2 (15), 2221-2223. https://doi.org/10.1021/ol000098m
  151. A. Gontcharov, H. Liu and K. B. Sharpless, Aminohydroxylation of Olefins with Tert-Alkyl Sulfonamides, U. S. Patent number 6,008,376, issued December 28, 1999.
  152. G. Li and K. B. Sharpless, Two Step Synthesis of D- and L- α-Amino Acids and D- and L- α-Amino-Aldehydes, U.S. Patent number 5,994,583, issued November 30, 1999.
  153. J. Rudolph and K. B. Sharpless, Accelerated Catalysis of Olefinic Epoxidations, U.S. Patent number 5,939,568, issued August 17, 1999.
  154. J. U. Jeong and K. B. Sharpless, Aziridination of Olefins, U.S. Patent number 5,929,252, issued July 27, 1999.
  155. Chuang, T.-H.; Sharpless, K. B., Applications of Aziridinium Ions. Selective Syntheses of Β-Aryl-Α,Β-Diamino Esters. Org. Lett. 1999, 1 (9), 1435-1437. https://doi.org/10.1021/ol990256d
  156. G. Li, H.-T. Chang and K. B. Sharpless, Catalytic Asymmetric Aminohydroxylation of Olefins with Sulfonamides, U.S. Patent number 5,859,281, issued January 12, 1999.
  157. Thomas, A. A.; Sharpless, K. B., The Catalytic Asymmetric Aminohydroxylation of Unsaturated Phosphonates. J. Org. Chem. 1999, 64 (22), 8379-8385. https://doi.org/10.1021/jo990060r
  158. Gontcharov, A. V.; Liu, H.; Sharpless, K. B., Tert-Butylsulfonamide. A New Nitrogen Source for Catalytic Aminohydroxylation and Aziridination of Olefins. Org. Lett. 1999, 1 (5), 783-786. https://doi.org/10.1021/ol990761a
  159. Pringle, W.; Sharpless, K. B., The Osmium-Catalyzed Aminohydroxylation of Baylis-Hillman Olefins. Tetrahedron Lett. 1999, 40 (28), 5151-5154. https://doi.org/10.1016/S0040-4039(99)00887-4
  160. Adolfsson, H.; Converso, A.; Sharpless, K. B., Comparison of Amine Additives Most Effective in the New Methyltrioxorhenium-Catalyzed Epoxidation Process. Tetrahedron Lett. 1999, 40(21), 3991-3994. https://doi.org/10.1016/S0040-4039(99)00661-9
  161. Goossen, L. J.; Liu, H.; Dress, R.; Sharpless, K. B., Catalytic Asymmetric Aminohydroxylation with Amino-Substituted Heterocycles as Nitrogen Sources. Angew. Chem., Int. Ed. 1999, 38(8), 1080-1083. https://doi.org/10.1002/(SICI)1521-3773(19990419)38:8<1080::AID-ANIE1080>3.0.CO;2-D
  162. G. Li and K. B. Sharpless, Catalytic Asymmetric Aminohydroxylation of Olefins with Carbamates, U.S. Patent number 5,767,304, issued June 16, 1998.
  163. Gypser, A.; Michel, D.; Nirschl, D. S.; Sharpless, K. B., Dihydroxylation of Polyenes Using Narasaka’s Modification of the Upjohn Procedure. J. Org. Chem. 1998, 63 (21), 7322-7327. https://doi.org/10.1021/JO980850L
  164. Dress, K. R.; Goossen, L. J.; Liu, H.; Jerina, D. M.; Sharpless, K. B., Catalytic Aminohydroxylation Using Adenine-Derivatives as the Nitrogen Source. Tetrahedron Lett. 1998, 39 (42), 7669-7672. https://doi.org/10.1016/S0040-4039(98)01716-X
  165. Jeong, J. U.; Tao, B.; Sagasser, I.; Henniges, H.; Sharpless, K. B., Bromine-Catalyzed Aziridination of Olefins. A Rare Example of Atom-Transfer Redox Catalysis by a Main Group Element. J. Am. Chem. Soc. 1998, 120 (27), 6844-6845. https://doi.org/10.1021/JA981419G
  166. Reddy, K. L.; Dress, K. R.; Sharpless, K. B., N-Chloro-N-Sodio-2-Trimethylsilyl Ethyl Carbamate: A New Nitrogen Source for the Catalytic Asymmetric Aminohydroxylation. Tetrahedron Lett. 1998, 39 (22), 3667-3670. https://doi.org/10.1016/S0040-4039(98)00644-3
  167. Tao, B.; Schlingloff, G.; Sharpless, K. B., Reversal of Regioselection in the Asymmetric Aminohydroxylation of Cinnamates. Tetrahedron Lett. 1998, 39 (17), 2507-2510. https://doi.org/10.1016/S0040-4039(98)00350-5
  168. Coperet, C.; Adolfsson, H.; Khuong, T.-A. V.; Yudin, A. K.; Sharpless, K. B., A Simple and Efficient Method for the Preparation of Pyridine N-Oxides. J. Org. Chem. 1998, 63 (5), 1740-1741. https://doi.org/10.1021/JO9723467
  169. Kolb, H. C.; Sharpless, K. B. In Asymmetric Aminohydroxylation, Wiley-VCH Verlag GmbH: 1998; pp 243-260.
  170. Kolb, H. C.; Sharpless, K. B. In Asymmetric Dihydroxylation, Wiley-VCH Verlag GmbH: 1998; pp 219-242.
  171. Coperet, C.; Adolfsson, H.; Chiang, J. P.; Yudin, A. K.; Sharpless, K. B., A Simple and Efficient Method for the Preparation of Pyridine N-Oxides. Ii. Tetrahedron Lett. 1998, 39 (8), 761-764. https://doi.org/10.1016/S0040-4039(97)10619-0
  172. Reddy, K. L.; Sharpless, K. B., From Styrenes to Enantiopure Α-Arylglycines in Two Steps. J. Am. Chem. Soc. 1998, 120 (6), 1207-1217. https://doi.org/10.1021/JA9728177
  173. DelMonte, A. J.; Haller, J.; Houk, K. N.; Sharpless, K. B.; Singleton, D. A.; Strassner, T.; Thomas, A. A., Experimental and Theoretical Kinetic Isotope Effects for Asymmetric Dihydroxylation. Evidence Supporting a Rate-Limiting “(3 + 2)” Cycloaddition. J. Am. Chem. Soc. 1997, 119 (41), 9907-9908. https://doi.org/10.1021/JA971650E
  174. Yudin, A. K.; Sharpless, K. B., Bis(Trimethylsilyl) Peroxide Extends the Range of Oxorhenium Catalysts for Olefin Epoxidation. J. Am. Chem. Soc. 1997, 119 (47), 11536-11537. https://doi.org/10.1021/JA973043X
  175. Rubin, A. E.; Sharpless, K. B., A Highly Efficient Aminohydroxylation Process. Angew. Chem., Int. Ed. Engl. 1997, 36 (23), 2637-2640. https://doi.org/10.1002/anie.199726371
  176. Coperet, C.; Adolfsson, H.; Sharpless, K. B., A Simple and Efficient Method for Epoxidation of Terminal Alkenes. Chem. Commun. (Cambridge) 1997, (16), 1565-1566. https://doi.org/10.1039/a703542j
  177. Rudolph, J.; Reddy, K. L.; Chiang, J. P.; Sharpless, K. B., Highly Efficient Epoxidation of Olefins Using Aqueous H2o2 and Catalytic Methyltrioxorhenium/Pyridine: Pyridine-Mediated Ligand Acceleration. J. Am. Chem. Soc. 1997, 119 (26), 6189-6190. https://doi.org/10.1021/JA970623L
  178. Bruncko, M.; Schlingloff, G.; Sharpless, K. B., N-Bromoacetamide – a New Nitrogen Source for the Catalytic Asymmetric Aminohydroxylation of Olefins. Angew. Chem., Int. Ed. Engl. 1997, 36 (13/14), 1483-1486. https://doi.org/10.1002/anie.199714831
  179. Nelson, D. W.; Gypser, A.; Ho, P. T.; Kolb, H. C.; Kondo, T.; Kwong, H.-L.; McGrath, D. V.; Rubin, A. E.; Norrby, P.-O.; Gable, K. P.; Sharpless, K. B., Toward an Understanding of the High Enantioselectivity in the Osmium-Catalyzed Asymmetric Dihydroxylation. 4. Electronic Effects in Amine-Accelerated Osmylations. J. Am. Chem. Soc. 1997, 119 (8), 1840-1858. https://doi.org/10.1021/JA961464T
  180. Vanhessche, K. P. M.; Sharpless, K. B., Catalytic Asymmetric Synthesis of New Halogenated Chiral Synthons. Chem. – Eur. J. 1997, 3 (4), 517-522. https://doi.org/10.1002/chem.19970030406
  181. Li, G.; Angert, H. H.; Sharpless, K. B., N-Halocarbamate Salts Lead to More Efficient Catalytic Asymmetric Aminohydroxylation. Angew. Chem., Int. Ed. Engl. 1997, 35 (23/24), 2813-2817. https://doi.org/10.1002/anie.199628131
  182. Oi, R.; Sharpless, K. B., 3-[(1s)-1,2-Dihydroxyethyl]-1,5-Dihydro-3h-2,4-Benzodioxepine (1,2-Ethanediol, 1-(1,5-Dihydro-2,4-Benzodioxepin-3-Yl)-, (S)-). Org. Synth. 1996, 73, 1-12. https://doi.org/10.15227/orgsyn.073.0001
  183. Rudolph, J.; Sennhenn, P. C.; Vlaar, C. P.; Sharpless, K. B., Smaller Substituents on Nitrogen Facilitate the Osmium-Catalyzed Asymmetric Aminohydroxylation. Angewandte Chemie International Edition in English 1996, 35 (23-24), 2810-2813. https://doi.org/10.1002/anie.199628101
  184. Vanhessche, K. P. M.; Sharpless, K. B., Ligand-Dependent Reversal of Facial Selectivity in the Asymmetric Dihydroxylation. J. Org. Chem. 1996, 61 (23), 7978-7979. https://doi.org/10.1021/JO961189T
  185. Chang, H.-T.; Sharpless, K. B., Molar Scale Synthesis of Enantiopure Stilbene Oxide. J. Org. Chem. 1996, 61 (18), 6456-6457. https://doi.org/10.1021/JO960718Q
  186. M. Beller and K.B. Sharpless, Diols Via Catalytic Dihydroxylation, “Applied Homogeneous Catalysis by Organometallic Complexes”, Boy Cornils and Wolfgang A. Herrmann. Eds.; VCH Publishers: 1996; pp 1009-1024.
  187. K.B. Sharpless, M. Beller, B. Blackburn, Y. Kawanami, H.-L. Kwong, Y. Ogino, T. Shibata, T. Ukita and L. Wang, Method For Catalytic Asymmetric Dihydroxylation of Olefins Using Heterocyclic Chiral Ligands, U.S. Patent 5,516,929, 1996 assigned to Massachusetts Institute of Technology.
  188. I.E. Marko and K. B. Sharpless, Ligand-Accelerated Catalytic Asymmetric Dihydroxylation, European Patent 0395729, 1996, assigned to Massachusetts Institute of Technology.
  189. Chang, H.-T.; Sharpless, K. B., A Practical Route to Enantiopure 1,2-Amino Alcohols. Tetrahedron Lett. 1996, 37 (19), 3219-3222. https://doi.org/10.1016/0040-4039(96)00534-5
  190. Li, G.; Sharpless, K. B., Catalytic Asymmetric Aminohydroxylation Provides a Short Taxol Side-Chain Synthesis. Acta Chem. Scand. 1996, 50 (8), 649-651. https://doi.org/10.3891/acta.chem.scand.50-0649
  191. Bruncko, M.; Khuong, T.-A. V.; Sharpless, K. B., Allylic Amination and 1,2-Diamination with a Modified Diimidoselenium Reagent. Angew. Chem., Int. Ed. Engl. 1996, 35 (4), 454-6. https://doi.org/10.1002/anie.199604541
  192. Li, G.; Chang, H.-T.; Sharpless, K. B., Catalytic Asymmetric Aminohydroxylation (AA) of Olefins. Angewandte Chemie International Edition in English 1996, 35 (4), 451-454. https://doi.org/10.1002/anie.199604511
  193. Becker, H.; Sharpless, K. B., A New Ligand Class for the Asymmetric Dihydroxylation of Olefins. Angew. Chem., Int. Ed. Engl. 1996, 35 (4), 448-51. https://doi.org/10.1002/anie.199604481
  194. Norrby, P.-O.; Becker, H.; Sharpless, K. B., Toward an Understanding of the High Enantioselectivity in the Osmium-Catalyzed Asymmetric Dihydroxylation. 3. New Insights into Isomeric Forms of the Putative Osmaoxetane Intermediate. J. Am. Chem. Soc. 1996, 118 (1), 35-42. https://doi.org/10.1021/JA952470C
  195. Chang, H.-T.; Chen, C.-T.; Kondo, T.; Siuzdak, G.; Sharpless, K. B., Asymmetric Dihydroxylation Enables Rapid Construction of Chiral Dendrimers Based on 1,2-Diols. Angew. Chem., Int. Ed. Engl. 1996, 35 (2), 182-6. https://doi.org/10.1002/anie.199601821
  196. Richardson, P. F.; Nelson, L. T. J.; Sharpless, K. B., Synthesis of Vicinal Diamines from Cyclic Sulfates. Tetrahedron Lett. 1995, 36 (51), 9241-4. https://doi.org/10.1016/0040-4039(95)02014-G
  197. Hugger, U.; Sharpless, K. B., Asymmetric Dihydroxylation Affords Enantiomerically Pure C12 Building Blocks from Trans,Trans,Cis-1,5,9-Cyclododecatriene. Tetrahedron Lett. 1995, 36(37), 6603-6. https://doi.org/10.1016/00404-0399(50)1365-O
  198. Becker, H.; King, S. B.; Taniguchi, M.; Vanhessche, K. P. M.; Sharpless, K. B., New Ligands and Improved Emantioselectivities for the Asymmetric Dihydroxylation of Olefins. J. Org. Chem. 1995, 60 (13), 3940-1. https://doi.org/10.1021/jo00118a005
  199. K.B. Sharpless and J.M. Klunder, Optically Active Derivatives of Glycidol, U.S. Patent 5,344,947, 1994 assigned to Massachusetts Institute of Technology.
  200. Berrisford, D. J.; Bolm, C.; Sharpless, K. B., Ligand-Accelerated Catalysis. Angew. Chem., Int. Ed. Engl. 1995, 34 (10), 1059-70. https://doi.org/10.1002/anie.199510591
  201. Becker, H.; Soler, M. A.; Sharpless, K. B., Selective Asymmetric Dihydroxylation of Polyenes. Tetrahedron 1995, 51 (5), 1345-76. https://doi.org/10.1016/0040-4020(94)01021-Q
  202. Wang, Z.-M.; Sharpless, K. B., A Solid-to-Solid Asymmetric Dihydroxylation Procedure for Kilogram-Scale Preparation of Enantiopure Hydrobenzoin. J. Org. Chem. 1994, 59 (26), 8302-3. https://doi.org/10.1021/jo00105a065
  203. Wang, Z.-M.; Kakiuchi, K.; Sharpless, K. B., Osmium-Catalyzed Asymmetric Dihydroxylation of Cyclic Cis-Disubstituted Olefins. J. Org. Chem. 1994, 59 (23), 6895-7. https://doi.org/10.1021/jo00102a008
  204. Kolb, H. C.; VanNieuwenhze, M. S.; Sharpless, K. B., Catalytic Asymmetric Dihydroxylation. Chem. Rev. (Washington, D. C.) 1994, 94 (8), 2483-547. https://doi.org/10.1021/cr00032a009
  205. Becker, H.; Ho, P. T.; Kolb, H. C.; Loren, S.; Norrby, P.-O.; Sharpless, K. B., Comparing Two Models for the Selectivity in the Asymmetric Dihydroxylation Reaction (AD). Tetrahedron Lett. 1994, 35 (40), 7315-18. https://doi.org/10.1016/0040-4039(94)85302-9
  206. Norrby, P.-O.; Kolb, H. C.; Sharpless, K. B., Toward an Understanding of the High Enantioselectivity in the Osmium-Catalyzed Asymmetric Dihydroxylation. 2. A Qualitative Molecular Mechanics Approach. J. Am. Chem. Soc. 1994, 116 (19), 8470-8. https://doi.org/10.1021/ja00098a006
  207. Bennani, Y. L.; Vanhessche, K. P. M.; Sharpless, K. B., A Short Route to a Moshe’rs Acid Precursor Via Catalytic Asymmetric Dihydroxylation (AD). Tetrahedron: Asymmetry 1994, 5 (8), 1473-1476. https://doi.org/10.1016/0957-4166(94)80116-9
  208. K.B. Sharpless and Y. Gao, Ruthenium-Catalyzed Production of Cyclic Sulfates, U.S. Patent 5,321,143, 1994 assigned to Massachusetts Institute of Technology.
  209. King, S. B.; Sharpless, K. B., An Efficient Synthesis of Enantiomerically Pure Trans-2-Phenylcyclohexanol. Tetrahedron Lett. 1994, 35 (31), 5611-12. https://doi.org/10.1016/S0040-4039(00)77259-5
  210. Wang, Z.-M.; Kolb, H. C.; Sharpless, K. B., Large-Scale and Highly Enantioselective Synthesis of the Taxol C-13 Side Chain through Asymmetric Dihydroxylation. J. Org. Chem. 1994, 59(17), 5104-5. https://doi.org/10.1021/jo00096a072
  211. Walsh, P. J.; Ho, P. T.; King, S. B.; Sharpless, K. B., Asymmetric Dihydroxylation of Olefins Containing Sulfur: Chemoselective Oxidation of C-C Double Bonds in the Presence of Sulfides, 1,3-Dithianes, and Disulfides. Tetrahedron Lett. 1994, 35 (29), 5129-32. https://doi.org/10.1016/S0040-4039(00)77045-6
  212. Xu, D.; Sharpless, K. B., Synthesis and Stereochemical Assignments for Goniobutenolides a and B. Tetrahedron Lett. 1994, 35 (27), 4685-8. https://doi.org/10.1016/S0040-4039(00)76941-3
  213. Vanhessche, K. P. M.; Wang, Z.-M.; Sharpless, K. B., Asymmetric Dihydroxylation of Primary Allylic Halides and a Concise Synthesis of (-)-Diepoxybutane. Tetrahedron Lett. 1994, 35 (21), 3469-72. https://doi.org/10.1016/S0040-4039(00)73212-6
  214. Xu, D.; Park, C. Y.; Sharpless, K. B., Study of the Regio- and Enantioselectivity of the Reactions of Osmium Tetroxide with Allylic Alcohols and Allylic Sulfonamides. Tetrahedron Lett. 1994, 35 (16), 2495-8. https://doi.org/10.1016/S0040-4039(00)77153-X
  215. Sharpless, K. B., Coelacanths and Catalysis. Tetrahedron 1994, 50 (15), 4235-58. https://doi.org/10.1016/S0040-4020(01)89364-9
  216. Kolb, H. C.; Andersson, P. G.; Sharpless, K. B., Toward an Understanding of the High Enantioselectivity in the Osmium-Catalyzed Asymmetric Dihydroxylation (Ad). 1. Kinetics. J. Am. Chem. Soc. 1994, 116 (4), 1278-91. https://doi.org/10.1021/ja00083a014
  217. VanNieuwenhze, M. S.; Sharpless, K. B., The Asymmetric Dihydroxylation Cis-Allylic and Homoallylic Alcohols. Tetrahedron Lett. 1994, 35 (6), 843-6. https://doi.org/10.1016/S0040-4039(00)75978-8
  218. Henderson, I.; Sharpless, K. B.; Wong, C. H., Synthesis of Carbohydrates Via Tandem Use of the Osmium-Catalyzed Asymmetric Dihydroxylation and Enzyme-Catalyzed Aldol Addition Reactions. J. Am. Chem. Soc. 1994, 116 (2), 558-61. https://doi.org/10.1021/ja00081a016
  219. Crispino, G. A.; Makita, A.; Wang, Z. M.; Sharpless, K. B., A Comparison of Ligands Proposed for Asymmetric Dihydroxylation. Tetrahedron Lett. 1994, 35 (4), 543-6. https://doi.org/10.1016/S0040-4039(00)75833-3
  220. Norrby, P. O.; Kolb, H. C.; Sharpless, K. B., Calculations on the Reaction of Ruthenium Tetroxide with Olefins Using Density Functional Theory (DFT). Implications for the Possibility of Intermediates in Osmium-Catalyzed Asymmetric Dihydroxylation. Organometallics 1994, 13 (1), 344-7. https://doi.org/10.1021/om00013a050
  221. Johnson, R. A.; Sharpless, K. B. In Catalytic Asymmetric Epoxidation of Allylic Alcohols, VCH: 1993; pp 103-58.
  222. Johnson, R. A.; Sharpless, K. B. In Catalytic Asymmetric Dihydroxylation, VCH: 1993; pp 227-22.
  223. Kalantar, T. H.; Sharpless, K. B., Transformations of Hydroxy Cyclic Sulfates: Stereospecific Conversion into 2,3,5-Trisubstituted Tetrahydrofurans. Acta Chem. Scand. 1993, 47 (3), 307-13. https://doi.org/10.3891/acta.chem.scand.47-0307
  224. Kolb, H. C.; Andersson, P. G.; Bennani, Y. L.; Crispino, G. A.; Jeong, K. S.; Kwong, H. L.; Sharpless, K. B., On “the Origin of High Enantioselectivity in the Dihydroxylation of Olefins Using Osmium Tetraoxide and Cinchona Alkaloid Catalysts”. J. Am. Chem. Soc. 1993, 115 (25), 12226-7. https://doi.org/10.1021/ja00078a096
  225. Amberg, W.; Bennani, Y. L.; Chadha, R. K.; Crispino, G. A.; Davis, W. D.; Hartung, J.; Jeong, K. S.; Ogino, Y.; Shibata, T.; Sharpless, K. B., Syntheses and Crystal Structures of the Cinchona Alkaloid Derivatives Used as Ligands in the Osmium-Catalyzed Asymmetric Dihydroxylation of Olefins. J. Org. Chem. 1993, 58 (4), 844-9. https://doi.org/10.1021/jo00056a015
  226. Wang, Z. M.; Sharpless, K. B., Asymmetric Dihydroxylation of Tertiary Allylic Alcohols. Tetrahedron Lett. 1993, 34 (51), 8225-8. https://doi.org/10.1016/S0040-4039(00)61396-5
  227. Arrington, M. P.; Bennani, Y. L.; Gobel, T.; Walsh, P.; Zhao, S. H.; Sharpless, K. B., Modified Cinchona Alkaloid Ligands: Improved Selectivities in the Osmium Tetroxide Catalyzed Asymmetric Dihydroxylation (AD) of Terminal Olefins. Tetrahedron Lett. 1993, 34 (46), 7375-8. https://doi.org/10.1016/S0040-4039(00)60129-6
  228. Morikawa, K.; Sharpless, K. B., Double Diastereoselection in Asymmetric Dihydroxylation. Tetrahedron Lett. 1993, 34 (35), 5575-8. https://doi.org/10.1016/S0040-4039(00)73885-8
  229. Morikawa, K.; Park, J.; Andersson, P. G.; Hashiyama, T.; Sharpless, K. B., Catalytic Asymmetric Dihydroxylation of Tetrasubstituted Olefins. J. Am. Chem. Soc. 1993, 115 (18), 8463-4. https://doi.org/10.1021/ja00071a072
  230. Walsh, P. J.; Bennani, Y. L.; Sharpless, K. B., Asymmetric Dihydroxylation (Ad)/Cyclization of N-Diboc Allylic and Homoallylic Amines: Selective Differentiation of the Hydroxyl Groups. Tetrahedron Lett. 1993, 34 (35), 5545-8. https://doi.org/10.1016/S0040-4039(00)73877-9
  231. McGrath, D. V.; Brabson, G. D.; Sharpless, K. B.; Andrews, L., Reinvestigation of the Infrared Spectra of Oxoosmium(Vi) Esters by Isotopic Labeling. Inorg. Chem. 1993, 32 (19), 4164-5. https://doi.org/10.1021/ic00071a035
  232. Crispino, G. A.; Sharpless, K. B., Enantioselective Synthesis of Juvenile Hormone Iii in Three Steps from Methyl Farnesoate. Synthesis 1993, (8), 777-9. https://doi.org/10.1055/s-1993-25939
  233. Walsh, P. J.; Sharpless, K. B., Asymmetric Dihydroxylation (AD) of Α,Β-Unsaturated Ketones. Synlett 1993, (8), 605-6. https://doi.org/10.1055/s-1993-22548
  234. Wang, Z. M.; Sharpless, K. B., Asymmetric Dihydroxylation of Α-Substituted Styrene Derivatives. Synlett 1993, (8), 603-4. https://doi.org/10.1055/s-1993-22547
  235. VanNieuwenhze, M. S.; Sharpless, K. B., Kinetic Resolution of Racemic Olefins Via Asymmetric Dihydroxylation. J. Am. Chem. Soc. 1993, 115 (17), 7864-5. https://doi.org/10.1021/ja00070a037
  236. Andersson, P. G.; Sharpless, K. B., A Dramatic Ligand Effect on the Relative Reactivities of Substituted Alkenes with Osmium Tetroxide. J. Am. Chem. Soc. 1993, 115 (15), 7047-8. https://doi.org:10.1021/ja00068a102
  237. Göbel, T.; Sharpless, K. B., Temperature Effects in Asymmetric Dihydroxylation: Evidence for a Stepwise Mechanism. Angewandte Chemie International Edition in English 1993, 32 (9), 1329-1331. https://doi.org/10.1002/anie.199313291
  238. Crispino, G. A.; Jeong, K. S.; Kolb, H. C.; Wang, Z. M.; Xu, D.; Sharpless, K. B., Improved Enantioselectivity in Asymmetric Dihydroxylations of Terminal Olefins Using Pyrimidine Ligands. J. Org. Chem. 1993, 58 (15), 3785-6. https://doi.org/10.1021/jo00067a002
  239. Okamoto, S.; Tani, K.; Sato, F.; Sharpless, K. B.; Zargarian, D., Synthesis of Optically Active Secondary Allylic Alcohols from Allylsilanes Via Successive Asymmetric Dihydroxylation (AD) and Peterson Olefination Reactions. Tetrahedron Lett. 1993, 34 (15), 2509-12. https://doi.org/10.1016/S0040-4039(00)60454-9
  240. Wang, Z. M.; Zhang, X. L.; Sharpless, K. B., Asymmetric Dihydroxylation of Aryl Allyl Ethers. Tetrahedron Lett. 1993, 34 (14), 2267-70. https://doi.org/10.1016/S0040-4039(00)77590-3
  241. Bennani, Y. L.; Sharpless, K. B., Asymmetric Synthesis of Γ-Hydroxy Α,Β-Unsaturated Amides Via an Asymmetric Dihydroxylation (AD)-Elimination Process; Synthesis of (+)-Coriolic Acid. Tetrahedron Lett. 1993, 34 (13), 2083-6. https://doi.org/10.1016/S0040-4039(00)60351-9
  242. Bennani, Y. L.; Sharpless, K. B., Asymmetric Dihydroxylation (AD) of N,N-Dialkyl and N-Methoxy-N-Methyl Α,Β- and Β,Γ-Unsaturated Amides. Tetrahedron Lett. 1993, 34 (13), 2079-82. https://doi.org/10.1016/S0040-4039(00)60350-7
  243. Xu, D.; Sharpless, K. B., A Simple Route to Enantiomerically Enriched Oxazolidin-2-Ones. Tetrahedron Lett. 1993, 34 (6), 951-2. https://doi.org/10.1016/S0040-4039(00)77462-4
  244. Kolb, H. C.; Bennani, Y. L.; Sharpless, K. B., Short and Practical Syntheses of (R)-(-)-Carnitine and (R)-(-)-Γ-Amino-Β-Hydroxybutyric Acid (Gabob). Tetrahedron: Asymmetry 1993, 4 (1), 133-41. https://doi.org/10.1016/S0957-4166(00)86023-1
  245. Crispino, G. A.; Sharpless, K. B., Enantioselective Synthesis of Both Enantiomers of 7,7-Dimethyl-6,8-Dioxabicyclo[3.2.1]Octane Via Regioselective Asymmetric Dihydroxylation. Synlett 1993, (1), 47-8. https://doi.org/10.1055/s-1993-22343
  246. Crispino, G. A.; Ho, P. T.; Sharpless, K. B., Selective Perhydroxylation of Squalene: Taming the Arithmetic Demon. Science (Washington, D. C., 1883-) 1993, 259 (5091), 64-6. https://doi.org/10.1126/science.8418495
  247. McKee, B. H.; Gilheany, D. G.; Sharpless, K. B., (R,R)-1,2-Diphenyl-1,2-Ethanediol (Stilbene Diol). Org. Synth. 1992, 70, 47-53. https://doi.org/10.15227/orgsyn.070.0047
  248. Kolb, H. C.; Sharpless, K. B., A Simplified Procedure for the Stereospecific Transformation of 1,2-Diols into Epoxides. Tetrahedron 1992, 48 (48), 10515-30. https://doi.org/10.1016/S0040-4020(01)88349-6
  249. Keinan, E.; Sinha, S. C.; Sinha-Bagchi, A.; Wang, Z. M.; Zhang, X. L.; Sharpless, K. B., Synthesis of All Four Isomers of Disparlure Using Osmium-Catalyzed Asymmetric Dihydroxylation. Tetrahedron Lett. 1992, 33 (43), 6411-14. https://doi.org/10.1016/S0040-4039(00)79002-2
  250. Wang, Z. M.; Zhang, X. L.; Sharpless, K. B.; Sinha, S. C.; Sinha-Bagchi, A.; Keinan, E., A General Approach to Γ-Lactones Via Osmium-Catalyzed Asymmetric Dihydroxylation. Synthesis of (-)- and (+)-Muricatacin. Tetrahedron Lett. 1992, 33 (43), 6407-10. https://doi.org/10.1016/S0040-4039(00)79001-0
  251. Hashiyama, T.; Morikawa, K.; Sharpless, K. B., Α-Hydroxy Ketones in High Enantiomeric Purity from Asymmetric Dihydroxylation of Enol Ethers. J. Org. Chem. 1992, 57 (19), 5067-8. https://doi.org/10.1021/jo00045a011
  252. Xu, D.; Crispino, G. A.; Sharpless, K. B., Selective Asymmetric Dihydroxylation (AD) of Dienes. J. Am. Chem. Soc. 1992, 114 (19), 7570-1. https://doi.org/10.1021/ja00045a043
  253. Wang, L.; Sharpless, K. B., Catalytic Asymmetric Dihydroxylation of Cis-Disubstituted Olefins. J. Am. Chem. Soc. 1992, 114 (19), 7568-70. https://doi.org/10.1021/ja00045a042
  254. Crispino, G. A.; Sharpless, K. B., Asymmetric Dihydroxylation of Squalene. Tetrahedron Lett. 1992, 33 (30), 4273-4. https://doi.org/10.1016/S0040-4039(00)74236-5
  255. Jeong, K. S.; Sjo, P.; Sharpless, K. B., Asymmetric Dihydroxylation of Enynes. Tetrahedron Lett. 1992, 33 (27), 3833-6. https://doi.org/10.1016/S0040-4039(00)74797-6
  256. Sharpless, K. B.; Amberg, W.; Bennani, Y. L.; Crispino, G. A.; Hartung, J.; Jeong, K. S.; Kwong, H. L.; Morikawa, K.; Wang, Z. M.; et, a., The Osmium-Catalyzed Asymmetric Dihydroxylation: A New Ligand Class and a Process Improvement. J. Org. Chem. 1992, 57 (10), 2768-71. https://doi.org/10.1021/jo00036a003
  257. Oi, R.; Sharpless, K. B., Asymmetric Dihydroxylation of Acrolein Acetals: Synthesis of Stable Equivalents of Enantiopure Glyceraldehyde and Glycidaldehyde. Tetrahedron Lett. 1992, 33(16), 2095-8. https://doi.org/10.1016/0040-4039(92)88149-Y
  258. McKee, B. H.; Kalantar, T. H.; Sharpless, K. B., Subtle Effects in the Asymmetric Epoxidation: Dependence of Kinetic Resolution Efficiency on the Monodentate Alkoxide Ligands of the Bystander Titanium Center. J. Org. Chem. 1991, 56 (25), 6966-8. https://doi.org/10.1021/jo00025a003
  259. Ogino, Y.; Chen, H.; Manoury, E.; Shibata, T.; Beller, M.; Lubben, D.; Sharpless, K. B., A Ligand Structure-Enantioselectivity Relationship for the Osmium Catalyzed Asymmetric Dihydroxylation of Olefins. Tetrahedron Lett. 1991, 32 (41), 5761-4. https://doi.org/10.1016/S0040-4039(00)93549-4
  260. Oi, R.; Sharpless, K. B., Facile Synthesis of Enantiopure Trans-2,3-Diphenyl-1,4-Diazabicyclo[2.2.2]Octane. Tetrahedron Lett. 1991, 32 (37), 4853-4. https://doi.org/10.1016/S0040-4039(00)93478-6
  261. Sharpless, K. B.; Amberg, W.; Beller, M.; Chen, H.; Hartung, J.; Kawanami, Y.; Lubben, D.; Manoury, E.; Ogino, Y.; et, a., New Ligands Double the Scope of the Catalytic Asymmetric Dihydroxylation of Olefins. J. Org. Chem. 1991, 56 (15), 4585-8. https://doi.org/10.1021/jo00015a001
  262. Ogino, Y.; Chen, H.; Kwong, H. L.; Sharpless, K. B., The Timing of Hydrolysis-Reoxidation in the Osmium-Catalyzed Asymmetric Dihydroxylation of Olefins Using Potassium Ferricyanide as the Reoxidant. Tetrahedron Lett. 1991, 32 (32), 3965-8. https://doi.org/10.1016/0040-4039(91)80601-2
  263. Park, C. Y.; Kim, B. M.; Sharpless, K. B., Catalytic Osmylation of Conjugated Dienes: A One-Pot Stereoselective Synthesis of Polyols. Tetrahedron Lett. 1991, 32 (8), 1003-6. https://doi.org/10.1016/S0040-4039(00)74472-8
  264. Oi, R.; Sharpless, K. B., Stereospecific Conversion of Chiral 1,2-Cyclic Sulfates to Chiral Imidazolines. Tetrahedron Lett. 1991, 32 (8), 999-1002. https://doi.org/10.1016/S0040-4039(00)74471-6
  265. Fleming, P. R.; Sharpless, K. B., Selective Transformations of Threo-2,3-Dihydroxy Esters. J. Org. Chem. 1991, 56 (8), 2869-75. https://doi.org/10.1021/jo00008a051
  266. Finn, M. G.; Sharpless, K. B., Mechanism of Asymmetric Epoxidation. 2. Catalyst Structure. J. Am. Chem. Soc. 1991, 113 (1), 113-26. https://doi.org/10.1021/ja00001a019
  267. Woodard, S. S.; Finn, M. G.; Sharpless, K. B., Mechanism of Asymmetric Epoxidation. 1. Kinetics. J. Am. Chem. Soc. 1991, 113 (1), 106-13. https://doi.org/10.1021/ja00001a018
  268. Johnson, R.A. and Sharpless, K.B., Addition Reactions with Formation of Carbon-Oxygen Bonds: (ii) Asymmetric Methods of Epoxidation, “Comprehensive Organic Synthesis,” Vol. 7, Barry M. Trost, Ed.; Pergamon Press: 1991; 389-436.
  269. K.B. Sharpless, J.M. Klunder, and T.H. Onami, Optically Active Derivatives of Glycidol, U. S. Patent 4,946,974, 1990 assigned to Massachusetts Institute of Technology.
  270. K.B. Sharpless and I.E. Markó, Ligand-Accelerated Catalytic Asymmetric Dihydroxylation, U.S. Patent 4,965,364, 1990 assigned to Massachusetts Institute of Technology.
  271. Moon Kim, B.; Barry Sharpless, K., A Short Route to Β-Lactams: Use of Cyclic Sulfites from Syn-2,3-Dihydroxy Esters. Tetrahedron Letters 1990, 31 (30), 4317-4320. https://doi.org/10.1016/S0040-4039(00)97610-X
  272. Shibata, T.; Gilheany, D. G.; Blackburn, B. K.; Sharpless, K. B., Ligand-Based Improvement of Enantioselectivity in the Catalytic Asymmetric Dihydroxylation of Dialkyl-Substituted Olefins. Tetrahedron Lett. 1990, 31 (27), 3817-20. https://doi.org/10.1016/S0040-4039(00)97477-X
  273. Ko, S. Y.; Lee, A. W. M.; Masamune, S.; Reed, L. A., III; Sharpless, K. B.; Walker, F. J., Total Synthesis of the L-Hexoses. Tetrahedron 1990, 46 (1), 245-64. https://doi.org/10.1016/S0040-4020(01)97596-9
  274. K.B. Sharpless, R. Hanson, and S.Y. Ko, Catalytic Asymmetric Epoxidation, U.S. Patent 4,900,847, 1990 assigned to the Massachusetts Institute of Technology.
  275. Moon Kim, B.; Sharpless, K. B., Heterogeneous Catalytic Asymmetric Dihydroxylation: Use of a Polymer-Bound Alkaloid. Tetrahedron Letters 1990, 31 (21), 3003-3006. https://doi.org/10.1016/S0040-4039(00)89009-7
  276. Hoi-Lun, K.; Sorato, C.; Ogino, Y.; Hou, C.; Barry Sharpless, K., Preclusion of the “Second Cycle” in the Osmium-Catalyzed Asymmetric Dihydroxylation of Olefins Leads to a Superior Process. Tetrahedron Letters 1990, 31 (21), 2999-3002. https://doi.org/10.1016/S0040-4039(00)89008-5
  277. Pearlstein, R. M.; Blackburn, B. K.; Davis, W. M.; Sharpless, K. B., Structural Characterization of the Pseudoenantiomeric Cis-Dioxo Osmium(Vi) Esters of Chiral Diols with Cinchona Alkaloid Ligands. Angewandte Chemie International Edition in English 1990, 29 (6), 639-641. https://doi.org/10.1002/anie.199006391
  278. Hayashi, M.; Okamura, F.; Toba, T.; Oguni, N.; Sharpless, K. B., Kinetic Resolution of Racemic Β-Hydroxy Amines by Enantioselective N-Oxide Formation. Chem. Lett. 1990, (4), 547-8. https://doi.org/10.1246/cl.1990.547
  279. K.B. Sharpless and I.E. Markó, Ligand-Accelerated Catalytic Asymmetric Dihydroxylation using Dihydroquinidine and Dihydroquinidine Esters as Ligands, U.S Patent 4,871,855, 1989 assigned to the Massachusetts Institute of Technology.
  280. Dijkstra, G. D. H.; Kellogg, R. M.; Wynberg, H.; Svendsen, J. S.; Marko, I.; Sharpless, K. B., Conformational Study of Cinchona Alkaloids. A Combined Nmr, Molecular Mechanics and X-Ray Approach. J. Am. Chem. Soc. 1989, 111 (21), 8069-76. https://doi.org/10.1021/ja00203a001
  281. Carlier, P. R.; Sharpless, K. B., Studies on the Mechanism of the Asymmetric Epoxidation: A Ligand Variation Approach. J. Org. Chem. 1989, 54 (17), 4016-18. https://doi.org/10.1021/jo00278a004
  282. Burns, C. J.; Martin, C. A.; Sharpless, K. B., Tartrate-Like Ligands in the Asymmetric Epoxidation. J. Org. Chem. 1989, 54 (12), 2826-34. https://doi.org/10.1021/jo00273a010
  283. Kim, B. M.; Sharpless, K. B., Cyclic Sulfates Containing Acid-Sensitive Groups and Chemoselective Hydrolysis of Sulfate Esters. Tetrahedron Lett. 1989, 30 (6), 655-8. https://doi.org/10.1016/S0040-4039(01)80274-4
  284. Bhushan Lohray, B.; Kalantar, T. H.; Moon Kim, B.; Park, C. Y.; Shibata, T.; Wai, J. S. M.; Barry Sharpless, K., Documenting the Scope of the Catalytic Asymmetric Dihydroxylation. Tetrahedron Letters 1989, 30 (16), 2041-2044. https://doi.org/10.1016/S0040-4039(01)93706-2
  285. Svendsen, J. S.; Marko, I.; Jacobsen, E. N.; Rao, C. P.; Bott, S.; Sharpless, K. B., The Structure of Osmium Tetraoxide-Cinchona Alkaloid Complexes. J. Org. Chem. 1989, 54 (10), 2263-4. https://doi.org/10.1021/jo00271a002
  286. Lohray, B. B.; Gao, Y.; Sharpless, K. B., One-Pot Synthesis of Homochiral Aziridines and Amino Alcohols from Homochiral 1,2-Cyclic Sulfates. Tetrahedron Lett. 1989, 30 (20), 2623-6. https://doi.org/10.1016/S0040-4039(00)99081-6
  287. Wai, J. S. M.; Marko, I.; Svendsen, J. S.; Finn, M. G.; Jacobsen, E. N.; Sharpless, K. B., A Mechanistic Insight Leads to a Greatly Improved Osmium-Catalyzed Asymmetric Dihydroxylation Process. J. Am. Chem. Soc. 1989, 111 (3), 1123-5. https://doi.org/10.1021/ja00185a050
  288. Jacobsen, E. N.; Marko, I.; France, M. B.; Svendsen, J. S.; Sharpless, K. B., Kinetic Role of the Alkaloid Ligands in Asymmetric Catalytic Dihydroxylation. J. Am. Chem. Soc. 1989, 111 (2), 737-9. https://doi.org/10.1021/ja00184a055
  289. Klunder, J. M.; Onami, T.; Sharpless, K. B., Arenesulfonate Derivatives of Homochiral Glycidol: Versatile Chiral Building Blocks for Organic Synthesis. J. Org. Chem. 1989, 54 (6), 1295. https://doi.org/10.1021/jo00267a014
  290. Bolm, C.; Davis, W. M.; Halterman, R. L.; Sharpless, K. B., Synthesis and Crystal Structure of a Chiral C3-Symmetric Monophosphane. Angewandte Chemie International Edition in English 1988, 27 (6), 835-837. https://doi.org/10.1002/anie.198808351
  291. Gao, Y.; Sharpless, K. B., Vicinal Diol Cyclic Sulfates. Like Epoxides Only More Reactive. J. Am. Chem. Soc. 1988, 110 (22), 7538-9. https://doi.org/10.1021/ja00230a045
  292. Bolm, C.; Sharpless, K. B., Synthesis of a C3-Symmetric Phospha[2.2.2]Cyclophane. Tetrahedron Lett. 1988, 29 (40), 5101-4. https://doi.org/10.1016/S0040-4039(00)80690-5
  293. Caron, M.; Carlier, P. R.; Sharpless, K. B., Regioselective Azide Opening of 2,3-Epoxy Alcohols by [Ti(O-I-Pr)2(N3)2]: Synthesis of Α-Amino Acids. J. Org. Chem. 1988, 53 (21), 5185-7. https://doi.org/10.1021/jo00256a063
  294. Gao, Y.; Sharpless, K. B., Asymmetric Synthesis of Both Enantiomers of Tomoxetine and Fluoxetine. Selective Reduction of 2,3-Epoxycinnamyl Alcohol with Red-Al. J. Org. Chem. 1988, 53 (17), 4081-4. https://doi.org/10.1021/jo00252a036
  295. Gao, Y.; Sharpless, K. B., Titanium Isopropoxide Mediated Formation of 2,3-Epithio Alcohols from 2,3-Epoxy Alcohols. J. Org. Chem. 1988, 53 (17), 4114-16. https://doi.org/10.1021/jo00252a046
  296. Bolm, C.; Davis, W. M.; Halterman, R. L.; Sharpless, K. B., Synthesis and Crystal Structure of a Chiral C3-Symmetric Monophosphane. Angewandte Chemie International Edition in English 1988, 27 (6), 835-837. https://doi.org/10.1002/anie.198808351
  297. Carlier, P. R.; Mungall, W. S.; Schroder, G.; Sharpless, K. B., Enhanced Kinetic Resolution and Enzyme-Like Shape Selectivity. J. Am. Chem. Soc. 1988, 110 (9), 2978-9. https://doi.org/10.1021/ja00217a052
  298. Sharpless, K. B., Catalytic Asymmetric Epoxidation. Janssen Chim. Acta 1988, 6 (1), 3-6.
  299. Jacobsen, E. N.; Marko, I.; Mungall, W. S.; Schroeder, G.; Sharpless, K. B., Asymmetric Dihydroxylation Via Ligand-Accelerated Catalysis. J. Am. Chem. Soc. 1988, 110 (6), 1968-70. https://doi.org/10.1021/ja00214a053
  300. Hawkins, J. M.; Sharpless, K. B., Asymmetric Epoxidation Models: An Alkyl Hydroperoxide Dependent Change in Mehanism. Tetrahedron Letters 1987, 28 (25), 2825-2828. https://doi.org/10.1016/S0040-4039(00)96219-1
  301. Klunder, J. M.; Sharpless, K. B., Convenient Synthesis of Sulfinate Esters from Sulfonyl Chlorides. J. Org. Chem. 1987, 52 (12), 2598-602. https://doi.org/10.1021/jo00388a051
  302. Pedersen, S. F.; Dewan, J. C.; Eckman, R. R.; Sharpless, K. B., Unexpected Diversity in the Coordination Chemistry of Tartrate Esters with Titanium(IV). J. Am. Chem. Soc. 1987, 109 (4), 1279-82. https://doi.org/10.1021/ja00238a065
  303. Elbein, A. D.; Szumilo, T.; Sanford, B. A.; Sharpless, K. B.; Adams, C., Effect of Isomers of Swainsonine on Glycosidase Activity and Glycoprotein Processing. Biochemistry 1987, 26 (9), 2502-10. https://doi.org/10.1021/bi00383a015
  304. Ko, S. Y.; Masamune, H.; Sharpless, K. B., P-Nitrobenzoate Esters of Epoxy Alcohols: Convenient Synthons for Water-Soluble Epoxy Alcohols. J. Org. Chem. 1987, 52 (4), 667-71. https://doi.org/10.1021/jo00380a032
  305. Sharpless, K. B., Architecturally Interesting Metal Complexes with Thermodynamically Dictated Structures. Chem. Scr. 1987, 27 (4), 521-4.
  306. Ko, S. Y.; Sharpless, K. B., In Situ Opening of Epoxy Alcohols: A Convenient Alternative to the Isolation of Unstable Epoxy Alcohols. J. Org. Chem. 1986, 51 (26), 5413-15. https://doi.org/10.1021/jo00376a068
  307. Gao, Y.; Klunder, J. M.; Hanson, R. M.; Masamune, H.; Ko, S. Y.; Sharpless, K. B., Catalytic Asymmetric Epoxidation and Kinetic Resolution: Modified Procedures Including in Situ Derivatization. J. Am. Chem. Soc. 1987, 109 (19), 5765-80. https://doi.org/10.1021/ja00253a032
  308. Kirshenbaum, K. S.; Sharpless, K. B., Regioselective Nucleophilic Opening of Erythro- and Threo-2,3-Epoxy Alcohols. Chem. Lett. 1987, (1), 11-14. https://doi.org/10.1246/cl.1987.11
  309. Klunder, J. M.; Ko, S. Y.; Sharpless, K. B., Asymmetric Epoxidation of Allyl Alcohol: Efficient Routes to Homochiral Β-Adrenergic Blocking Agents. J. Org. Chem. 1986, 51 (19), 3710-12. https://doi.org/10.1021/jo00369a032
  310. Bartmann, W.; Sharpless, K. B.; Editors, Stereochemistry of Organic and Bioorganic Transformations. [Proceedings of the 17th Workshop Conference Hoechst, Schloss Reisensburg, 8-11 October 1986]. VCH: 1987; p 330 pp
  311. K.B. Sharpless and R.A. Johnson, Metal-Mediated Halohydrin Formation, U. S. Patent 4,560,811, 1985, assigned to the Massachusetts Institute of Technology.
  312. Hanson, R. M.; Sharpless, K. B., Procedure for the Catalytic Asymmetric Epoxidation of Allylic Alcohols in the Presence of Molecular Sieves. J. Org. Chem. 1986, 51 (10), 1922-5. https://doi.org/10.1021/jo00360a058
  313. Sharpless, K. B., The Discovery of the Asymmetric Epoxidation. Chem. Br. 1986, 22 (1), 38-40, 43-4.
  314. Hawkins, J. M.; Dewan, J. C.; Sharpless, K. B., Dioxomolybdenum(Vi)-Substituted 2,6-Pyridinedimethanol Complexes: New Five-Coordinate Species. Inorg. Chem. 1986, 25 (9), 1501-3. https://doi.org/10.1021/ic00229a041
  315. Hill, J. G.; Sharpless, K. B.; Exon, C. M.; Regenye, R., Enantioselective Epoxidation of Allylic Alcohols: (2s,3s)-3-Propyloxiranemethanol (Oxiranemethanol, 3-Propyl-, (2s,3s)-). Org. Synth. 1985, 63, 66-78. https://doi.org/10.15227/orgsyn.063.0066
  316. Sharpless, K. B., The Discovery of Titanium-Catalyzed Asymmetric Epoxidation. CHEMTECH 1985, 15 (11), 692-700.
  317. T. Katsuki and K.B. Sharpless, Method for Asymmetric Epoxidation, U.S. Patent 4,471,130, 1984, assigned to Stanford University.
  318. Behrens, C. H.; Sharpless, K. B., Selective Transformations of 2,3-Epoxy Alcohols and Related Derivatives. Strategies for Nucleophilic Attack at Carbon-3 or Carbon-2. J. Org. Chem. 1985, 50 (26), 5696-704. https://doi.org/10.1021/jo00350a051
  319. Behrens, C. H.; Ko, S. Y.; Sharpless, K. B.; Walker, F. J., Selective Transformation of 2,3-Epoxy Alcohols and Related Derivatives. Strategies for Nucleophilic Attack at Carbon-1. J. Org. Chem. 1985, 50 (26), 5687-96. https://doi.org/10.1021/jo00350a050
  320. Chong, J. M.; Sharpless, K. B., Regioselective Openings of 2,3-Epoxy Acids with Organocuprates. Tetrahedron Lett. 1985, 26 (39), 4683-6. https://doi.org/10.1016/S0040-4039(00)94923-2
  321. Miyano, S.; Lu, L. D. L.; Viti, S. M.; Sharpless, K. B., Kinetic Resolution of Racemic Β-Hydroxy Amines by Enantioselective N-Oxide Formation. J. Org. Chem. 1985, 50 (22), 4350-60. https://doi.org/10.1021/jo00222a030
  322. Chong, J. M.; Sharpless, K. B., Nucleophilic Opening of 2,3-Epoxy Acids and Amides Mediated by Titanium Isopropoxide. Highly Enhanced C-3 Selectivity. J. Org. Chem. 1985, 50 (9), 1560-3. https://doi.org/10.1021/jo00209a048
  323. Caron, M.; Sharpless, K. B., Titanium Isopropoxide-Mediated Nucleophilic Openings of 2,3-Epoxy Alcohols. A Mild Procedure for Regioselective Ring-Opening. J. Org. Chem. 1985, 50 (9), 1557-60. https://doi.org/10.1021/jo00209a047
  324. Schweiter, M. J.; Sharpless, K. B., The Asymmetric Epoxidation of Tert-Butyl Substituted Allylic Alcohols. Tetrahedron Lett. 1985, 26 (21), 2543-6. https://doi.org/10.1016/S0040-4039(00)98832-4
  325. Kirshenbaum, K. S.; Sharpless, K. B., Improved Procedure for the Tungstate-Catalyzed Epoxidation of Α,Β-Unsaturated Acids. J. Org. Chem. 1985, 50 (11), 1979-82. https://doi.org/10.1021/jo00211a040
  326. Klunder, J. M.; Caron, M.; Uchiyama, M.; Sharpless, K. B., Chlorohydroxylation of Olefins with Peroxides and Titanium Tetrachloride. J. Org. Chem. 1985, 50 (6), 912-15. https://doi.org/10.1021/jo00206a048
  327. Finn, M. G.; Sharpless, K. B. In On the Mechanism of Asymmetric Epoxidation with Titanium-Tartrate Catalysts, Academic: 1985; pp 247-308.
  328. Adams, C. E.; Walker, F. J.; Sharpless, K. B., Enantioselective Synthesis of Swainsonine, a Trihydroxylated Indolizidine Alkaloid. J. Org. Chem. 1985, 50 (3), 420-2. https://doi.org/10.1021/jo00203a039
  329. Williams, I. D.; Pedersen, S. F.; Sharpless, K. B.; Lippard, S. J., Crystal Structures of Two Titanium Tartrate Asymmetric Epoxidation Catalysts. J. Am. Chem. Soc. 1984, 106 (21), 6430-1. https://doi.org/10.1021/ja00333a060
  330. Hawkins, J. M.; Sharpless, K. B., Threo-N,N’-Bis(Α-Methylbenzyl)Sulfamide: A Readily Available Chiral Ligand for Asymmetric Lithium Aluminum Hydride Reductions. J. Org. Chem. 1984, 49 (20), 3861-2. https://doi.org/10.1021/jo00194a048
  331. Rossiter, B. E.; Sharpless, K. B., Asymmetric Epoxidation of Homoallylic Alcohols. Synthesis of (-)-Γ-Amino-Β-(R)-Hydroxybutyric Acid (Gabob). J. Org. Chem. 1984, 49 (20), 3707-11. https://doi.org/10.1021/jo00194a007
  332. Sharpless, K. B., Discovery of the Titanium-Catalyzed Asymmetric Epoxidation – a Personal Account. Proc. Robert A. Welch Found. Conf. Chem. Res. 1984, 27, 59-89.
  333. Lu, L. D. L.; Johnson, R. A.; Finn, M. G.; Sharpless, K. B., Two New Asymmetric Epoxidation Catalysts. Unusual Stoichiometry and Inverse Enantiofacial Selection. J. Org. Chem. 1984, 49(4), 728-31. https://doi.org/10.1021/jo00178a039
  334. Behrens, C. H.; Sharpless, K. B., New Transformations of 2,3-Epoxy Alcohols and Related Derivatives. Easy Routes to Homochiral Substances. Aldrichimica Acta 1983, 16 (4), 67-80.
  335. Sharpless, K. B.; Woodard, S. S.; Finn, M. G., On the Mechanism of Titanium-Tartrate Catalyzed Asymmetric Epoxidation. Pure Appl. Chem. 1983, 55 (11), 1823-36. https://doi.org/10.1351/pac198355111823
  336. Miyano, S.; Lu, L. D. L.; Viti, S. M.; Sharpless, K. B., Kinetic Resolution of Racemic Β-Hydroxy Amines by Enantioselective N-Oxide Formation. J. Org. Chem. 1983, 48 (20), 3608-11. https://doi.org/10.1021/jo00168a064
  337. Hill, J. G.; Rossiter, B. E.; Sharpless, K. B., Anhydrous Tert-Butyl Hydroperoxide in Toluene: The Preferred Reagent for Applications Requiring Dry Tbhp. J. Org. Chem. 1983, 48 (20), 3607-8. https://doi.org/10.1021/jo00168a063
  338. Ko, S. Y.; Lee, A. W. M.; Masamune, S.; Reed, L. A., III; Sharpless, K. B.; Walker, F. J., Total Synthesis of the L-Hexoses. Science (Washington, D. C., 1883-) 1983, 220 (4600), 949-51. https://doi.org/10.1126/science.220.4600.949
  339. Herranz, E.; Sharpless, K. B., Osmium-Catalyzed Vicinal Oxyamination of Olefins by N-Chloro-N-Argentocarbamates: Ethyl Threo-[1-(2-Hydroxy-1,2-Diphenylethyl)]Carbamate. [Carbamic Acid, (2-Hydroxy-1,2-Diphenylethyl)-, Ethyl Ester, (R*R*)-]. Org. Synth. 1983, 61, 93. https://doi.org/10.15227/orgsyn.061.0093
  340. Herranz, E.; Sharpless, K. B., Osmium-Catalyzed Vicinal Hydroxyamination of Olefins by Chloramine-T: Cis-2-(P-Toluenesulfonamido)Cyclohexanol and 2-Methyl-3-(P-Toluenesulfonamido)-2-Pentanol. [Benzenesulfonamide, N-(2-Hydroxycyclohexyl)-4-Methyl-, Cis-]. Org. Synth. 1983, 61, 85-93. https://doi.org/10.15227/orgsyn.061.0085
  341. Reed, L. A., III; Ito, Y.; Masamune, S.; Sharpless, K. B., Synthesis of Saccharides and Related Polyhydroxylated Natural Products. 4. Α-D- and Β-D-C-Glycopyranosides (2,6-Dialkyl-Substituted Tetrahydropyrans). J. Am. Chem. Soc. 1982, 104 (23), 6468-70. https://doi.org/10.1021/ja00387a062
  342. Sharpless, K. B.; Behrens, C. H.; Katsuki, T.; Lee, A. W. M.; Martin, V. S.; Takatani, M.; Viti, S. M.; Walker, F. J.; Woodard, S. S., Stereo and Regioselective Openings of Chiral 2,3-Epoxy Alcohols. Versatile Routes to Optically Pure Natural Products and Drugs. Unusual Kinetic Resolutions. Pure Appl. Chem. 1983, 55 (4), 589-604. https://doi.org/10.1351/pac198855040589
  343. Gonnella, N. C.; Nakanishi, K.; Martin, V. S.; Sharpless, K. B., General Method for Determining Absolute Configuration of Acyclic Allylic Alcohols. J. Am. Chem. Soc. 1982, 104 (13), 3775-6. https://doi.org/10.1021/ja00377a063
  344. Warpehoski, M. A.; Chabaud, B.; Sharpless, K. B., Selenium Dioxide Oxidation of Endocyclic Olefins. Evidence for a Dissociation-Recombination Pathway. J. Org. Chem. 1982, 47 (15), 2897-900. https://doi.org/10.1021/jo00136a017
  345. Lee, A. W. M.; Martin, V. S.; Masamune, S.; Sharpless, K. B.; Walker, F. J., Synthesis of Saccharides and Related Polyhydroxylated Natural Products. 3. Efficient Conversion of 2,3-Erythro-Aldoses to 2,3-Threo-Aldoses. J. Am. Chem. Soc. 1982, 104 (12), 3515-16. https://doi.org/10.1021/ja00376a050
  346. Ma, P.; Martin, V. S.; Masamune, S.; Sharpless, K. B.; Viti, S. M., Synthesis of Saccharides and Related Polyhydroxylated Natural Products. 2. Simple Deoxyalditols. J. Org. Chem. 1982, 47(7), 1378-80. https://doi.org/10.1021/jo00346a052
  347. Katsuki, T.; Lee, A. W. M.; Ma, P.; Martin, V. S.; Masamune, S.; Sharpless, K. B.; Tuddenham, D.; Walker, F. J., Synthesis of Saccharides and Related Polyhydroxylated Natural Products. 1. Simple Alditols. J. Org. Chem. 1982, 47 (7), 1373-8. https://doi.org/10.1021/jo00346a051
  348. Martin, V. S.; Woodard, S. S.; Katsuki, T.; Yamada, Y.; Ikeda, M.; Sharpless, K. B., Kinetic Resolution of Racemic Allylic Alcohols by Enantioselective Epoxidation. A Route to Substances of Absolute Enantiomeric Purity? J. Am. Chem. Soc. 1981, 103 (20), 6237-40. https://doi.org/10.1021/ja00410a053
  349. Umbreit, M. A.; Sharpless, K. B., Deoxygenation of Epoxides with Lower Valent Tungsten Halides: Trans-Cyclododecene. Org. Synth. 1981, 60, 29-34. https://doi.org/10.15227/orgsyn.060.0029
  350. Carlsen, P. H. J.; Katsuki, T.; Martin, V. S.; Sharpless, K. B., A Greatly Improved Procedure for Ruthenium Tetroxide Catalyzed Oxidations of Organic Compounds. J. Org. Chem. 1981, 46(19), 3936-8. https://doi.org/10.1021/jo00332a045
  351. Morgans, D. J., Jr.; Sharpless, K. B.; Traynor, S. G., Epoxy Alcohol Rearrangements: Hydroxyl-Mediated Delivery of Lewis Acid Promoters. J. Am. Chem. Soc. 1981, 103 (2), 462-4. https://doi.org/10.1021/ja00392a037
  352. Rossiter, B. E.; Katsuki, T.; Sharpless, K. B., Asymmetric Epoxidation Provides Shortest Routes to Four Chiral Epoxy Alcohols Which Are Key Intermediates in Syntheses of Methymycin, Erythromycin, Leukotriene C-1, and Disparlure. J. Am. Chem. Soc. 1981, 103 (2), 464-5. https://doi.org/10.1021/ja00392a038
  353. Katsuki, T.; Sharpless, K. B., The First Practical Method for Asymmetric Epoxidation. J. Am. Chem. Soc. 1980, 102 (18), 5974-6. https://doi.org/10.1021/ja00538a077
  354. Hentges, S. G.; Sharpless, K. B., Improved Procedure for the Oxyamination of Olefins with Trioxo(Tert-Butylimido)Osmium(Viii). J. Org. Chem. 1980, 45 (11), 2257-9. https://doi.org/10.1021/jo01299a045
  355. Hentges, S. G.; Sharpless, K. B., Asymmetric Induction in the Reaction of Osmium Tetroxide with Olefins. J. Am. Chem. Soc. 1980, 102 (12), 4263-5. https://doi.org/10.1021/ja00532a050
  356. Herranz, E.; Sharpless, K. B., Osmium-Catalyzed Vicinal Oxyamination of Olefins by N-Chloro-N-Metallocarbamates. J. Org. Chem. 1980, 45 (13), 2710-13. https://doi.org/10.1021/jo01301a033
  357. Sharpless, K. B.; Verhoeven, T. R., Metal-Catalyzed, Highly Selective Oxygenations of Olefins and Acetylenes with Tert-Butyl Hydroperoxide. Practical Considerations and Mechanisms. Aldrichimica Acta 1979, 12 (4), 63-74.
  358. Rossiter, B. E.; Verhoeven, T. R.; Sharpless, K. B., Stereoselective Epoxidation of Acyclic Allylic Alcohols. A Correction of Our Previous Work. Tetrahedron Lett. 1979, (49), 4733-6. https://doi.org/10.1016/S0040-4039(01)86696-X
  359. Chabaud, B.; Sharpless, K. B., Oxidation of Acetylenes with Tert-Butyl Hydroperoxide Catalyzed by Selenium Dioxide. Α,Α’-Dioxygenation of Internal Alkynes. J. Org. Chem. 1979, 44(23), 4202-4. https://doi.org/10.1021/jo01337a045
  360. Hori, T.; Sharpless, K. B., Selenium-Catalyzed Nonradical Chlorination of Olefins with N-Chlorosuccinimide. J. Org. Chem. 1979, 44 (23), 4204-8. https://doi.org/10.1021/jo01337a046
  361. Hori, T.; Sharpless, K. B., Conversion of Allylic Phenylselenides to the Rearranged Allylic Chlorides by N-Chlorosuccinimide. Mechanism of Selenium-Catalyzed Allylic Chlorination of Β-Pinene. J. Org. Chem. 1979, 44 (23), 4208-10. https://doi.org/10.1021/jo01337a047
  362. Baeckvall, J. E.; Oshima, K.; Palermo, R. E.; Sharpless, K. B., Some Reactions of N-(2-Hydroxyalkyl)-P-Toluenesulfonamides and N-Allyl-P-Toluenesulfonamides. J. Org. Chem. 1979, 44(12), 1953-7. https://doi.org/10.1021/jo01326a013
  363. Current, S.; Sharpless, K. B., Carbonyl Participation in the Addition of P-Chlorophenylselenenyl Bromide to (E)-4-Hexenal: A New Route to 2,6-Dideoxyglycosides. Tetrahedron Lett. 1978, (51), 5075-8. https://doi.org/10.1016/S0040-4039(01)85816-0
  364. Liebeskind, L. S.; Sharpless, K. B.; Wilson, R. D.; Ibers, J. A., The First D0 Metallooxaziridines. Amination of Olefins. J. Am. Chem. Soc. 1978, 100 (22), 7061-3. https://doi.org/10.1021/ja00490a047
  365. Herranz, E.; Biller, S. A.; Sharpless, K. B., Osmium-Catalyzed Vicinal Oxyamination of Olefins by N-Chloro-N-Argentocarbamates. J. Am. Chem. Soc. 1978, 100 (11), 3596-8. https://doi.org/10.1021/ja00479a051
  366. Herranz, E.; Sharpless, K. B., Improvements in the Osmium-Catalyzed Oxyamination of Olefins by Chloramine-T. J. Org. Chem. 1978, 43 (12), 2544-8. https://doi.org/10.1021/jo00406a057
  367. Frejd, T.; Sharpless, K. B., A New Rearrangement of N-Arylhydroxamic Acids Catalyzed by Seleninic Acids and Phenylselenenyl Chloride. Tetrahedron Lett. 1978, (26), 2239-42. https://doi.org/10.1016/S0040-4039(01)91501-1
  368. Patrick, D. W.; Truesdale, L. K.; Biller, S. A.; Sharpless, K. B., Stereospecific Vicinal Oxyamination of Olefins by Alkylimidoosmium Compounds. J. Org. Chem. 1978, 43 (13), 2628-38. https://doi.org/10.1021/jo00407a016
  369. Akashi, K.; Palermo, R. E.; Sharpless, K. B., A Major Improvement in the Osmium Catalyzed Vicinal Hydroxylation of Olefins by Tert-Butyl Hydroperoxide. J. Org. Chem. 1978, 43 (10), 2063-6. https://doi.org/10.1021/jo00404a052
  370. Hori, T.; Sharpless, K. B., Synthetic Applications of Arylselenenic and Arylseleninic Acids. Conversion of Olefins to Allylic Alcohols and Epoxides. J. Org. Chem. 1978, 43 (9), 1689-97. https://doi.org/10.1021/jo00403a015
  371. Singer, S. P.; Sharpless, K. B., Synthesis of Dl-Gabaculine Utilizing Direct Allylic Amination as the Key Step. J. Org. Chem. 1978, 43 (7), 1448-55. https://doi.org/10.1021/jo00401a034
  372. Hori, T.; Singer, S. P.; Sharpless, K. B., Allylic Deuteration and Tritiation of Olefins with N-Sulfinylsulfonamides. J. Org. Chem. 1978, 43 (7), 1456-9. https://doi.org/10.1021/jo00401a035
  373. Baeckvall, J. E.; Young, M. W.; Sharpless, K. B., Vicinal Acetoxychlorination of Olefins by Chromyl Chloride in Acetyl Chloride. Tetrahedron Lett. 1977, (40), 3523-6. https://doi.org/10.1016/S0040-4039(01)83282-2
  374. Umbreit, M. A.; Sharpless, K. B., Allylic Oxidation of Olefins by Catalytic and Stoichiometric Selenium Dioxide with Tert-Butyl Hydroperoxide. J. Am. Chem. Soc. 1977, 99 (16), 5526-8. https://doi.org/10.1021/ja00458a072
  375. Chong, A. O.; Oshima, K.; Sharpless, K. B., Synthesis of Dioxobis(Tert-Alkylimido)Osmium(VIII) and Oxotris(Tert-Alkylimido)Osmium(VIII) Complexes. Stereospecific Vicinal Diamination of Olefins. J. Am. Chem. Soc. 1977, 99 (10), 3420-6. https://doi.org/10.1021/ja00452a039
  376. Sharpless, K. B.; Teranishi, A. Y.; Backvall, J. E., Chromyl Chloride Oxidations of Olefins. Possible Role of Organometallic Intermediates in the Oxidations of Olefins by Oxo Transition Metal Species. J. Am. Chem. Soc. 1977, 99 (9), 3120-8. https://doi.org/10.1021/ja00451a043
  377. Chong, A. O.; Sharpless, K. B., Mechanism of the Molybdenum and Vanadium Catalyzed Epoxidation of Olefins by Alkyl Hydroperoxides. J. Org. Chem. 1977, 42 (9), 1587-90. https://doi.org/10.1021/jo00429a024
  378. Michaelson, R. C.; Palermo, R. E.; Sharpless, K. B., Chiral Hydroxamic Acids as Ligands in the Vanadium Catalyzed Asymmetric Epoxidation of Allylic Alcohols by Tert-Butyl Hydroperoxide. J. Am. Chem. Soc. 1977, 99 (6), 1990-2. https://doi.org/10.1021/ja00448a059
  379. Sharpless, K. B.; Singer, S. P., 1,2-Diamination of 1,3-Dienes by Imido Selenium Compounds. J. Org. Chem. 1976, 41 (14), 2504-6. https://doi.org/10.1021/jo00876a040
  380. Sharpless, K. B.; Akashi, K.; Oshima, K., Ruthenium-Catalyzed Oxidation of Alcohols to Aldehydes and Ketones by Amine-N-Oxides. Tetrahedron Lett. 1976, (29), 2503-6. https://doi.org/10.1016/S0040-4039(00)78130-5
  381. Sharpless, K. B.; Akashi, K., Osmium Catalyzed Vicinal Hydroxylation of Olefins by Tert-Butyl Hydroperoxide under Alkaline Conditions. J. Am. Chem. Soc. 1976, 98 (7), 1986-7. https://doi.org/10.1021/ja00423a067
  382. Sharpless, K. B.; Chong, A. O.; Oshima, K., Osmium-Catalyzed Vicinal Oxyamination of Olefins by Chloramine-T. J. Org. Chem. 1976, 41 (1), 177-9. https://doi.org/10.1021/jo00863a052
  383. Sharpless, K. B.; Hori, T., Allylic Amination of Olefins and Acetylenes by Imido Sulfur Compounds. J. Org. Chem. 1976, 41 (1), 176-7. https://doi.org/10.1021/jo00863a051
  384. Sharpless, K. B.; Gordon, K. M., Selenium Dioxide Oxidation of Ketones and Aldehydes. Evidence for the Intermediacy of Β-Ketoseleninic. J. Am. Chem. Soc. 1976, 98 (1), 300-1. https://doi.org/10.1021/ja00417a083
  385. Sharpless, K. B.; Hori, T.; Truesdale, L. K.; Dietrich, C. O., Allylic Amination of Olefins and Acetylenes by Imido Selenium Compounds. J. Am. Chem. Soc. 1976, 98 (1), 269-71. https://doi.org/10.1021/ja00417a062
  386. Sharpless, K. B.; Akashi, K., Oxidation of Alcohols to Aldehydes by Reagents Derived from Chromyl Chloride. J. Am. Chem. Soc. 1975, 97 (20), 5927-8. https://doi.org/10.1021/ja00853a055
  387. Sharpless, K. B.; Gordon, K. M.; Lauer, R. F.; Patrick, D. W.; Singer, S. P.; Young, M. W., The Utility of Selenium Reagents in Organic Synthesis. Chem. Scr. 1975, 8A, 9-13.
  388. Nelson, J. A.; Kahn, S.; Spencer, T. A.; Sharpless, K. B.; Clayton, R. B., Some Aspects of Substrate Specificity in Biological Demethylation at C4 of Steroids. Bioorg. Chem. 1975, 4 (4), 363-76. https://doi.org/10.1016/0045-2068(75)90047-4
  389. Sharpless, K. B.; Williams, D. R., Reactions of Olefins with Permanganate, Ruthenium Tetroxide, and Osmium Tetroxide. Dependence of Rate on Degree of Substitution. Tetrahedron Lett. 1975, (35), 3045-6. https://doi.org/10.1016/S0040-4039(00)75068-4
  390. Sharpless, K. B.; Chong, A. O.; Scott, J. A., Rapid Separation of Organic Mixtures by Formation of Metal Complexes. J. Org. Chem. 1975, 40 (9), 1252-7. https://doi.org/10.1021/jo00897a015
  391. Sharpless, K. B.; Patrick, D. W.; Truesdale, L. K.; Biller, S. A., New Reaction. Stereospecific Vicinal Oxyamination of Olefins by Alkyl Imido Osmium Compounds. J. Am. Chem. Soc. 1975, 97 (8), 2305-7. https://doi.org/10.1021/ja00841a071
  392. Sharpless, K. B.; Young, M. W., Olefin Synthesis. Rate Enhancement of the Elimination of Alkyl Aryl Selenoxides by Electron-Withdrawing Substituents. J. Org. Chem. 1975, 40 (7), 947-9. https://doi.org/10.1021/jo00895a030
  393. Jensen, H. P.; Sharpless, K. B., Selenium Dioxide Oxidation of D-Limonene. Reinvestigation. J. Org. Chem. 1975, 40 (2), 264-5. https://doi.org/10.1021/jo00890a030
  394. Jensin, H. P.; Sharpless, K. B., Improved Procedure for the Direct Oxidation of Olefins to Α-Diketones by Potassium Permanganate in Acetic Anhydride. J. Org. Chem. 1974, 39 (15), 2314. https://doi.org/10.1021/jo00929a050
  395. Sharpless, K. B.; Jensen, H. P., Synthesis of a Novel Pentacoordinate Glyoxime-Based Ligand and Preparation of Its Chlorocobalt(Iii) Complex. Inorg. Chem. 1974, 13 (11), 2617-20. https://doi.org/10.1021/ic50141a017
  396. Tanaka, S.; Yamamoto, H.; Nozaki, H.; Sharpless, K. B.; Michaelson, R. C.; Cutting, J. D., Stereoselective Epoxidations of Acyclic Allylic Alcohols by Transition Metal-Hydroperoxide Reagents. Synthesis of Dl-C18 Cecropia Juvenile Hormone from Farnesol. J. Am. Chem. Soc. 1974, 96 (16), 5254-5. https://doi.org/10.1021/ja00823a042
  397. Sharpless, K. B.; Lauer, R. F., Electrophilic Organoselenium Reagents. New Route to Allylic Acetates and Ethers. J. Org. Chem. 1974, 39 (3), 429-30. https://doi.org/10.1021/jo00917a038
  398. Arigoni, D.; Vasella, A.; Sharpless, K. B.; Jensen, H. P., Selenium Dioxide Oxidations of Olefins. Trapping of the Allylic Seleninic Acid Intermediate as a Seleninolactone. J. Amer. Chem. Soc. 1973, 95 (23), 7917-19. https://doi.org/10.1021/ja00804a087
  399. Sharpless, K. B.; Lauer, R. F.; Teranishi, A. Y., Electrophilic and Nucleophilic Organoselenium Reagents. New Routes to Α,Β-Unsaturated Carbonyl Compounds. J. Amer. Chem. Soc. 1973, 95 (18), 6137-9. https://doi.org/10.1021/ja00799a062
  400. Sharpless, K. B.; Michaelson, R. C., High Stereo- and Regioselectivities in the Transition Metal Catalyzed Epoxidations of Olefinic Alcohols by Tert-Butyl Hydroperoxide. J. Amer. Chem. Soc. 1973, 95 (18), 6136-7. https://doi.org/10.1021/ja00799a061
  401. Sharpless, K. B.; Young, M. W.; Lauer, R. F., Reactions of Selenoxides. Thermal Syn-Elimination and Oxygen-18 Labeled Water Exchange. Tetrahedron Lett. 1973, (22), 1979-82. https://doi.org/10.1016/S0040-4039(01)96098-8
  402. Sharpless, K. B.; Lauer, R. F., Mild Procedure for the Conversion of Epoxides to Allylic Alcohols. First Organoselenium Reagent. J. Amer. Chem. Soc. 1973, 95 (8), 2697-9. https://doi.org/10.1021/ja00789a055
  403. Sharpless, K. B.; Teranishi, A. Y., Chromyl Chloride in Acetone. Α-Chloro Ketones and Ketones Directly from Olefins. J. Org. Chem. 1973, 38 (1), 185-6. https://doi.org/10.1021/jo00941a054
  404. Sharpless, K. B.; Lauer, R. F., Facile Thermal Rearrangements of Allyl Selenides and Diselenides. [1,3] and [2,3] Shifts. J. Org. Chem. 1972, 37 (24), 3973-4. https://doi.org/10.1021/jo00797a058
  405. Sharpless, K. B.; Lauer, R. F., Selenium Dioxide Oxidation of Olefins. Evidence for the Intermediacy of Allylseleninic Acids. J. Amer. Chem. Soc. 1972, 94 (20), 7154-5. https://doi.org/10.1021/ja00775a050
  406. Townsend, J. M.; Sharpless, K. B., Mechanism of Decomposition of Sulfonium Betaines to Epoxides. Tetrahedron Lett. 1972, (32), 3313-16. https://doi.org/10.1016/S0040-4039(01)94031-6
  407. Sharpless, K. B.; Umbreit, M. A.; Nieh, M. T.; Flood, T. C., Lower Valent Tungsten Halides. New Class of Reagents for Deoxygenation of Organic Molecules. J. Amer. Chem. Soc. 1972, 94(18), 6538-40. https://doi.org/10.1021/ja00773a045
  408. Sharpless, K. B.; Flood, T. C., Direct Deoxygenation of Vicinal Diols with Tungsten(Iv). New Olefin Synthesis. J. Chem. Soc., Chem. Commun. 1972, (7), 370-1. https://doi.org/10.1039/c39720000370
  409. Sharpless, K. B.; Townsend, J. M.; Williams, D. R., Mechanism of Epoxidation of Olefins by Covalent Peroxides of Molybdenum(Vi). J. Amer. Chem. Soc. 1972, 94 (1), 295-6. https://doi.org/10.1021/ja00756a062
  410. Sharpless, K. B.; Lauer, R. F.; Repic, O.; Teranishi, A. Y.; Williams, D. R., Permanganate in Acetic Anhydride. Α-Diketones Directly from Olefins. J. Amer. Chem. Soc. 1971, 93 (13), 3303-4. https://doi.org/10.1021/ja00742a045
  411. Sharpless, K. B.; Flood, T. C., Oxotransition Metal Oxidants as Mimics for the Action of Mixed-Function Oxygenases. “Nih Shift” with Chromyl Reagents. J. Amer. Chem. Soc. 1971, 93 (9), 2316-18. https://doi.org/10.1021/ja00738a039
  412. Sharpless, K. B., D,1-Malabaricanediol. First Cyclic Natural Product Derived from Squalene in a Nonenzymic Process. J. Amer. Chem. Soc. 1970, 92 (23), 6999-7001. https://doi.org/10.1021/ja00726a064
  413. Sharpless, K. B., Synthesis of Erythro-18,19-Dihydroxysqualene 2,3-Oxide and Other Internally Oxidized Squalene Derivatives. J. Chem. Soc. D 1970, (21), 1450-1. https://doi.org/10.1039/c29700001450
  414. Rahman, R.; Sharpless, K. B.; Spencer, T. A.; Clayton, R. B., Removal of the 4,4-Dimethyl Carbons in the Enzymic Conversion of Lanosterol to Cholesterol: Initial Loss of the 4α-Methyl Group. Journal of Biological Chemistry 1970, 245 (10), 2667-2671. https://doi.org/10.1016/S0021-9258(18)63121-7
  415. Sharpless, K. B.; Snyder, T. E.; Spencer, T. A.; Maheshwari, K. K.; Nelson, J. A.; Clayton, R. B., Biological Demethylation of 4,4-Dimethyl Sterols. Evidence for Enzymic Epimerization of the 4β-Methyl Group Prior to Its Oxidative Removal. J. Amer. Chem. Soc. 1969, 91 (12), 3394-6. https://doi.org/10.1021/ja01040a065
  416. Anderson, R. J.; Hanzlik, R. P.; Sharpless, K. B.; van Tamelen, E. E.; Clayton, R. B., Enzymic Transformation of an Acyclic Sesterterpene Terminal Epoxide into a Lanosterol Analogue. Journal of the Chemical Society D: Chemical Communications 1969, (2), 53-54. https://doi.org/10.1039/C29690000053
  417. Van Tamelen, E. E.; Akermark, B.; Sharpless, K. B., Mechanism of the Titanium-Promoted Deoxygenative Coupling of Allyl and Benzyl Alcohols to Hydrocarbons. J. Amer. Chem. Soc. 1969, 91 (6), 1552-4. https://doi.org/10.1021/ja01034a058
  418. Sharpless, K. B.; Van Tamelen, E. E., Terpene Terminal Epoxides. Skeletal Rearrangement Accompanying Bicyclization of Squalene 2,3-Oxide. J. Amer. Chem. Soc. 1969, 91 (7), 1848-9. https://doi.org/10.1021/ja01035a043
  419. Sharpless, K. B.; Snyder, T. E.; Spencer, T. A.; Maheshwari, K. K.; Guhn, G.; Clayton, R. B., Biological Demethylation of 4,4-Dimethyl Sterols. Initial Removal of the 4α-Methyl Group. J. Amer. Chem. Soc. 1968, 90 (24), 6874-5. https://doi.org/10.1021/ja01026a073
  420. Sharpless, K. B. Studies of the Mechanism of Action of 2,3-Oxidosqualene-Lanosterol Cyclase: Featuring Enzymic Cyclization of Modified Squalene Oxide. Ph.D. Dissertation, Stanford University 1968.
  421. Van Tamelen, E. E.; Hanzlik, R. P.; Sharpless, K. B.; Clayton, R. B.; Richter, W. J.; Burlingame, A. L., Enzymic Cyclization of 15-Norsqualene 2,3-Oxide. J. Amer. Chem. Soc. 1968, 90 (12), 3284-6. https://doi.org/10.1021/ja01014a081
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