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Solid-phase synthesis of benzisothiazolones as serine protease inhibitors
K L Yu1, R Civiello, D G Roberts
1Bristol-Myers Squibb Pharmaceutical Research Institute, Department of Chemistry, Wallingford, CT 06492, USA.
Bioorganic & Medicinal Chemistry Letters
|April 14, 1999
Abstract:
An efficient solid-phase synthesis of benzisothiazolone-1,1-dioxide-based serine protease inhibitors involving alkylation of carboxylic acids with N-(bromomethyl)benzisothiazolone-1,1-dioxide has been developed. An example using this procedure for preparation of a library of human mast cell tryptase inhibitors is described.