Source: Interfolio F180
Karl Sharpless
Research Focus
Designing Man-Made Catalysts
The Sharpless Lab pursues useful new reactivity and general methods for selectively controlling chemical reactions. Though the focus has progressed from regio- to stereo- to asymmetric and, now, to connectivity control, the core chemistry remains unchanged: the oxidation of olefins, that single most versatile, powerful and reliable (KBS argues) chemical transformation. The Sharpless Lab was the first academic chemistry group with robotics, and the lesson from the combinatorial numbers game was the primacy of reliability. "Click" chemistry was the Sharpless Lab's response: a set of powerful, virtually 100% reliable, selective reactions for the rapid synthesis of new compounds via heteroatom links (C-X-C). Click chemistry is integral now to all research within the Sharpless Lab.
In 2002, the Sharpless group discovered CuAAC (the copper-catalyzed azide-alkyne cycloaddition), now known as a quintessential 'click chemistry'. Recently the Sharpless group discovered SuFEx, another near-perfect click reaction. In concert with the thiol-ene reaction, these three make click chemistry a far-reaching method for drug discovery, chemical biology and materials science.
Education
B.A. (Chemistry), Dartmouth College, 1963Ph.D. (Chemistry), Stanford University, 1968
Awards & Professional Activities
1963 Hartshorn Chemistry Medal, Dartmouth College1983 Award for Creative Work in Synthetic Organic Chemistry, American Chemical Society
1986 Arthur C. Cope Scholar Award, American Chemical Society
1987 Harrison Howe Award, American Chemical Society, Rochester Section
1988 Chemical Pioneer Award, American Institute of Chemists
1988 Vladimir Prelog Medal for Stereochemistry, ETH
1989 Ira Remsen Award, American Chemical Society, Maryland Section
1989 Smissman Medal, University of Kansas
1991 Scheele Medal, Swedish Academy of Pharmaceutical Sciences
1992 Arthur C. Cope Scholar Award, American Chemical Society
1992 San Diego Scientist of the Year, American Chemical Society
1993 Tetrahedron Prize for Creativity in Organic Synthesis, Tetrahedron Publications
1993 Centenary Lecture Medalist, Royal Society of Chemistry
1994 World's Most Cited Scientists in Chemistry/Materials Science, Science World
1995 Honorary Doctorate, Dartmouth College
1995 Honorary Doctorate, Technical University of Munich
1995 Honorary Doctorate, Royal Institute of Technology, Stockholm
1995 King Faisal International Prize in Science, King Faisal Foundation
1995 World's Most Cited Scientists in Chemistry/Materials Science, Science World
1996 Honorary Doctorate, Catholic University of Louvain, Belgium
1996 World's Most Cited Scientists in Chemistry/Materials Science, Science World
1997 Honorary Fellow, Royal Society of Chemistry, Great Britain
1997 Roger Adams Award in Organic Chemistry, American Chemical Society
1997 Microbial Chemistry Medal, Kitasato Institute, Tokyo
1997 World's Most Cited Scientists in Chemistry/Materials Science, Science World
1998 Theodore William Richards Medal, American Chemical Society, Northeastern Section
Wallace Carothers Award
1998 Top 25 Contributors to the Chemical Enterprise, C&EN 75th birthday issue
1998 Harvey Science and Technology Prize, Israel Institute of Technology (Technion)
1999 Honorary Doctorate, Wesleyan University
2000 Paul N. Rylander Award, Organic Reactions Catalysis Society
2000 Rhone Poulenc Medal, Royal Society of Chemistry
2000 Chemical Sciences Award, National Academy of Sciences
2000 Chirality Medal, Italian Chemical Society
2001 Benjamin Franklin Medal, Franklin Institute, Philadelphia
2001 Inaugural Member, ISI Highly Cited Researchers Database
2001 Sharpless Tribute Symposia, American Chemical Society, San Diego
2001 Wolf Prize in Chemistry, Weizmann Institute, Tel Aviv
2001 John Scott Medal Award, City of Philadelphia
2001 Nobel Prize in Chemistry
2002 Honorary Member, Kitasato Institute
2002 Distinguished Honorary Professor, Hong Kong Polytechnic University
2004 Honorary Doctorate, National Taiwan Normal University, Taipei
2004 Honorary Professor & Member, Academic Committee, Shanghai Institute of Organic Chemistry
2005 Gold Medal of Cornelius University, Cornelius University, Bratislava, Slovakia
2005 Rama Rao-Hamied Award Lecture, Indian Institute of Chemical Technology, Hyderabad
2006 William H. Nichols Medalist, American Chemical Society, New York Section
2007 Honorary Doctorate, Hong Kong University of Science and Technology
2008 Honorary Professor, Nanjing University
2008 Breakthrough Award Citation, History of Chemistry Division, American Chemical Society
2009 World's 7 Most Powerful Innovators, Forbes Magazine
2010 Distinguished University Professor, Kyushu University, Japan
2010 Honorary Professor, Tianjin University
2010 José Medal of Honor, Institute of Chemistry of São Carlos, University of São Paulo, Brazil
2011 Honorary Professor, Soochow University, Suzhou, China
2011 Honorary Fellow, University of Florida
2011 Top 100 Chemists: 2000-2010 by Citation Impact, Thomson Reuters
2011 Top 100 Chemists, Thomas Reuters
2011 Andrew D. Dorsey Memorial Award, University of California at Berkeley
2012 Honorary Professor, Nankai University, Tianjin, China
2014 F.A. Cotton Medal, American Chemical Society, Texas A&M Section
2016 Click Chemistry Symposium in Honor of Professor Sharpless' 75th Birthday, American Chemical Society national meeting, San Diego
2019 Priestley Medal, American Chemical Society
2020 International Friendship Prize, Chinese Academy of Sciences
Selected Publications
Qin, H. L.; Zheng, Q.; Bare, G. A.; Wu, P.; Sharpless, K. B. A Heck-Matsuda process for the synthesis of ß-arylethenesulfonyl fluorides: selectively addressable bis-electrophiles for SuFEx click chemistry. Angewandte Chemie-International Edition 2016, 55, 14155-14158.
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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. 2016, 138, 7353-64.
Dong, J.; Krasnova, L.; Finn, M. G.; Sharpless, K. B. Sulfur(VI) fluoride exchange (SuFEx): another good reaction for click chemistry. Angewandte Chemie-International Edition 2014, 53, 9430-9448.
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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. 2013, 135, 5656-68.
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. Proceedings of the National Academy of Sciences of the United States of America 2013, 110, 15892-15897.
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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.; Sharpless, K. B.; Eckmann, L. Expanded therapeutic potential in activity space of next-generation 5-nitroimidazole antimicrobials with broad structural diversity. Proceedings of the National Academy of Sciences of the United States of America 2013, 110, 17564-17569.
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