第 38 卷第 4 期 Vol. 38 No. 4 2008 年 8 月 Aug 2008

所属栏目：医药及中间体 盐酸哌罗匹隆的合成工艺改进

潘 毅，陈 蔚，陶 勇 （天津药物研究院，天津 300193）

摘　要：以顺-六氢邻苯二甲酰亚胺（2）为起始原料，经多步反应合成盐酸哌罗匹隆（1）。中间体3-（哌嗪-1-基）-1，2-苯并异噻唑（9）的制备采用吡啶做催化剂，收率从文献的56.5％提高到71.4％。总收率从文献的46.4％提高到60.27％。合成的盐酸哌罗匹隆经 1H NMR、13C NMR、MS确证结构。该合成工艺原料价廉易得、操作简便、不需过柱分离，适合工业化生产。

关键词：工艺改进；哌罗匹隆；非典型抗精神病药物

中图分类号：R971+.41　　文献标识码：A　　文章编号：1009-9212（2008）04- 0031-03

An Improved Synthesis of Perospirone Hydrochloride

PAN Yi，CHEN Wei，TAO Yong （Tianjin Institute of Pharmaceutical Research，Tianjin 300193，China）

Abstract：Perospirone hydrochloride hydrate was synthesized through multistep reactions with cis-4-tetrahydrophthalimide as starting materia. 1，3-（piperazin-1-yl）-1，2-benzisothiazole was synthesized using pyridine as the promoter and its yield was improved from 56.5％ to 71.4％. The overall yield was improved from 46.4％ to 60.27％ and its structure was identified by 1H NMR，13C NMR and MS． In view of the cheap available materials and simple operations without colunm chromatograph，this synthetic process is suitable for large-scale manufacture.

Key words：proces improvement；perospirone；atypical antipsychotic agent

作者简介：潘 毅（1973-），男，天津人，助理研究员，主要从事药物合成研究。（E-mail：panyi1973@sina.com）

收稿日期： 2008-06-3