Effective synthesis of 1,5-disubstituted 2,1-benzisothiazol-3(1H)-ones

Abstract

A convenient and effective synthesis of novel 1,5-disubstituted 2,1-benzisothiazol-3(1H)-one derivatives is described. The approach involves nitration of inexpensive isatoic anhydride followed by its conversion to 5-nitro-2,1-benzisothiazol-3(1H)-ones in excellent yield and alkylation at the 1-position. The 5-amino group was further derivatized. © 2011 Taylor & Francis Group, LLC.