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he 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.
Improved osmium catalysts for epoxidation and aziridination; new strategies for asymmetric epoxidation and dihydroxylation
via osmium and rhenium catalysts New ligands for asymmetric catalysis (with TSRI chemist M. G. Finn) Highly connective in situ chemistries replacing traditional carbon frames (e.g. in drugs) with nitrogen networks Further study of acetyl cholinesterase inhibitors created during in situ assembly’s proof of concept (with TSRI chemists
M. G. Finn and F. Grynszpan and UCSD neuropharmacologist P. W. Taylor) Neurogeneration agents for Huntington’s Disease; compound libraries synthesized for screening by the Hereditary Disease Foundation, Los Angeles Drugs for oncogene-based human cancers (with TSRI oncovirologist P. K. Vogt) HIV protease inhibitors synthesized in situ (with TSRI molecular biologists J. H. Elder and A. J. Olson) Further study of powerful fibrile (plaque) formation inhibitors for Alzheimer’s Disease whose rapid discovery was
via click chemistry (with TSRI chemist J. W. Kelly)
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