Dartmouth College, Hanover, NH – B.A. 1963; Chemistry major
Stanford University, Stanford, CA – Ph.D. 1968; Organic Chemistry
Stanford University, Stanford, CA – NIH postdoc 1968-69; Organometallic Chemistry
Harvard University, Cambridge, MA – NIH postdoc 1699-70; Enzymology
Research Background
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 nearperfect 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.
Positions
1970-1990 Massachusetts Institute of Technology (MIT): Assistant Professor of Chemistry, 1970-1974; Associate Professor of Chemistry, 1974-1975; Professor of Chemistry, 1975-77, 1980-87; Arthur C. Cope Professor of Chemistry, 1987-1990
1977-1980 Stanford University, Professor of Chemistry
1990-present The Scripps Research Institute (TSRI), W.M. Keck Professor of Chemistry
1996-present Skaggs Institute for Chemical Biology of TSRI, Member
Honors
1983 Creative Work Award in Organic Synthesis, American Chemical Society (ACS)
1984 American Academy of Arts and Sciences, elected Member
1985 National Academy of Sciences, elected Member; Allan R. Day Award, Phil Organic Chemists Club
1986 Dr. Paul Janssen Prize for Creativity in Organic Synthesis, Belgium
1987 Simon Guggenheim Found Fellow; Harrison Howe Award, Rochester Section, ACS
1988 Rolf Sammet Prize, Johann Wolfgang Goethe Universität, Frankfurt-am-Main; Chemical Pioneer
Award, American Institute of Chemists
1988 Prelog Medal, Eidgenössische Technische Hochschule, Zürich
1989 Remsen Award, Maryland Section, ACS
1991 Scheele Medal, Swedish Academy of Pharmaceutical Sciences
1992 Arthur C. Cope Award, ACS
1993 Tetrahedron Prize for Creativity in Organic Chemistry
1995 The King Faisal International Prize for Science; Honorary Doctorates: Dartmouth College, Swedish
Royal Institute of Technology and Technische Universität München
1996 Honorary Doctorate, Université Catholique de Louvain, Belgium
1997 Roger Adams Award in Organic Chemistry, ACS; Microbial Chemistry Medal, The Kitosato Institute,
Tokyo, Japan
1998 Top 75 Contributors to the Chemical Enterprise, Chemical & Engineering News; Richards Medal,
Northeastern Section, ACS; Honorary Fellow of the Royal Society of Chemistry (Great Britain); Harvey
Prize in Science and Technology, Technion Israel Institute of Technology
1999 Carothers Award, Delaware Section, ACS; Honorary Degree, Wesleyan University
2000 Rylander Award, Organic Reactions Catalysis Society; Chemical Sciences Award, National Academy of
Sciences; Chiralty Medal, Italian Chemical Society; Rhone Poulenc Medal, Royal Society of Chemistry
2001 Nobel Prize in Chemistry (with Knowles & Noyori), Nobel Foundation; Benjamin Franklin Medal,
Franklin Institute, Philadelphia; Wolf Prize (with Kagan & Noyori), Wolf Foundation; John Scott Medal
Award, City of Philadelphia
2002 Distinguished Professor (Hon), Hong Kong Polytechnic University; Member (Hon), Kitasato Institute,
Japan
2008 Honorary Doctorate, Hong Kong University of Science and Technology, Hong Kong
Recent Publications
1. Zhang, E., Tang, J., Li, S., Wu, P., Moses, J. E., Sharpless, K. B. Chemoselective synthesis of
polysubstituted pyridines from heteroaryl fluorosulfates Chemistry-a European Journal 2016 22:5692-
5697 DOI:10.1002/chem.201600167 PMID:26990693
2. Bourne, Y., Sharpless, K. B., Taylor, P., Marchot, P. Steric and dynamic parameters influencing in situ cycloadditions to form triazole inhibitors with crystalline acetylcholinesterase Journal of the American Chemical Society 2016 138:1611-1621 DOI:10.1021/jacs.5b11384 PMID:26731630
3. 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 Angewandte Chemie-International Edition 2016 55:1835-1838 DOI:10.1002/anie.201509016 PMID: 26696445
4. 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., et al. A fluorogenic aryl fluorosulfate for intraorganellar transthyretin imaging in living cells and in Caenorhabditis elegans Journal of the American Chemical Society 2015 137:7404-414 DOI:10.1021/jacs.5b03042 PMID:26051248 PMCID:PMC4472559
5. 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 Organic Letters 2015 17:1942-
1945 DOI:10.1021/acs.orglett.5b00654 PMID:25856416
K. B. Sharpless
