Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.

K L Yu, R Civiello, D G Roberts, S M Seiler, N A Meanwell

Index: Bioorg. Med. Chem. Lett. 9(5) , 663-6, (1999)

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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.