New Disulfide Route to 3-(1-Piperazinyl)-1, 2-benzisothiazole. Nucleus for Atypical Antipsychotic Drugs

SW Walinsky, DE Fox, JF Lambert…

Index: Walinsky, Stanley W.; Fox, Darrell E.; Lambert, John F.; Sinay, Terry G. Organic Process Research and Development, 1999 , vol. 3, # 2 p. 126 - 130

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Citation Number: 10

Abstract

A new, one-step commercial process for the preparation of 3-(1-piperazinyl)-1, 2- benzisothiazole hydrochloride, a key intermediate for the syntheses of some new,“atypical antipsychotic” drugs, was developed. Reaction of bis (2-cyanophenyl) disulfide with excess piperazine at 120-140° C for 3-24 h in the presence of small amounts of DMSO and 2- propanol formed 3-(1-piperazinyl)-1, 2-benzisothiazole in 75-80% yields. The DMSO ...