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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 41, 2011 - Issue 22
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Original Articles

Effective Synthesis of 1,5-Disubstituted 2,1-Benzisothiazol-3(1H)-ones

, , , , , , , & show all
Pages 3265-3279 | Received 01 Apr 2010, Published online: 26 Jul 2011
 

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.

ACKNOWLEDGMENT

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

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