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Click here for an ever-growing compilation of click chemistry papers.
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 Sulfur(VI) Fluoride Exchange (SuFEx) transformations (with TSRI biochemist Peng Wu)

  • Highly connective in situ chemistries replacing traditional carbon frames (e.g. in drugs) with nitrogen networks

  • Covalent drugs via SuFEx for human cancers and immune disorders (with TSRI biochemists J. W. Kelly and Peng Wu)

  • Further study of acetyl cholinesterase inhibitors created during in situ assembly's proof of concept (with UCSD neuropharmacologist P. W. Taylor)

  • 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)

  • Functionalized polymers for biosensors and memory devices via SuFEx (with TSRI biochemist Peng Wu)

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