- Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.
Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.
Bioorganic & medicinal chemistry letters (1999-04-14)
K L Yu, R Civiello, D G Roberts, S M Seiler, N A Meanwell
PMID10201825
摘要
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.