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Chemical reagent speeds drug synthesis

NSF Award:

Application of Sulfinamides in Synthesis and Catalysis  (Yale University)

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A decade of NSF funding has enabled researchers to develop a chemical reagent that permits rapid, cost-effective preparation of amine-containing compounds. Drug structures previously difficult to prepare are now efficiently and reliably synthesized because of tert-butanesulfinamide (TBS). 

Amines are present in a large majority of drugs and drug candidates and many biologically active natural products. TBS makes it possible for pharmaceutical and biotechnology companies to prepare thousands of drug candidates for biological testing. Preclinical evaluation and clinical trials have also used TBS.

More than 100 chemical supply companies sell the reagent due to its importance to the pharmaceutical, agrochemical and biotechnology industries. In addition, industry has filed 700 patent applications citing TBS as a key reagent for the preparation or large-scale production of drug candidates.

NSF funding supported research into methods to prepare TBS in large quantities, TBS characterization and exploration of the chemical reactivity, and the development of widely used, TBS-based chemical synthesis methods. 

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  • graphic shows the many applications of TBS in drug development
The many applications of TBS in drug development.
Jonathan A. Ellman, Yale University

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