Yu K L, Civiello R, Roberts D G, Seiler S M, Meanwell N A
Bristol-Myers Squibb Pharmaceutical Research Institute, Department of Chemistry, Wallingford, CT 06492, USA.
Bioorg Med Chem Lett. 1999 Mar 8;9(5):663-6. doi: 10.1016/s0960-894x(99)00078-5.
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.
