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.

Keywords:

• 1,2-Benzisothiazol-3(2H)-one
• 2,1-benzoisothiazolin-3(1H)-one
• nitration
• sodium hydrogen sulfide

ACKNOWLEDGMENT

We are thankful to the Zydus management and analytical department for the support.