Solid-phase synthesis of benzisothiazolones as serine protease inhibitors

Authors
Yu, KL Civiello, R Roberts, DGM Seiler, SM Meanwell, NA
Citation
Kl. Yu et al., Solid-phase synthesis of benzisothiazolones as serine protease inhibitors, BIOORG MED, 9(5), 1999, pp. 663-666
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
663 - 666
Database
ISI
SICI code
0960-894X(19990308)9:5<663:SSOBAS>2.0.ZU;2-K
Abstract
An efficient solid-phase synthesis of benzisothiazolone-1,1-dioxide-based s erine protease inhibitors involving alkylation of carboxylic acids with N-( bromomethyl)benzisothiazolone-1,1-dioxide has been developed. An example us ing this procedure for preparation of a library of human mast cell tryptase inhibitors is described. (C) 1999 Elsevier Science Ltd. All rights reserve d.