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西他列汀侧链哌嗪盐酸盐制备的工艺优化
引用本文:唐红,贺银翠,张义长.西他列汀侧链哌嗪盐酸盐制备的工艺优化[J].云南化工,2019(7).
作者姓名:唐红  贺银翠  张义长
作者单位:铜仁学院材料与化学工程学院
摘    要:为了提高西他列汀侧链哌嗪盐酸盐的产率,并简化操作,以三氟乙酸乙酯为原料,经肼解、氧氯化磷环合、乙二胺亲核取代、闭环等反应,制备了3-(三氟甲基)-5,6,7,8-四氢1,2,4]三唑并4,3-α]哌嗪盐酸盐。工艺产物收率较高,反应条件温和,操作简单,溶剂回收简单。

关 键 词:3-(三氟甲基)-5  6  7  8-四氢[1  2  4]三唑并[4  3-α]哌嗪盐酸盐  西他列汀侧链哌嗪盐酸盐  工艺优化

Process optimization of sitagliptin side chain piperazine hydrochloride preparation
Affiliation:,College of Material and Chemical Engineering of Tongren University
Abstract:In order to improve the yield of side chain piperazine hydrochloride of statin and simplify the operation. In this study, 3-(trifluoromethyl)-5,6,7,8-tetrahydro 1,2,4] triazolo 4,3-a] piperazine hydrochloride was prepared from ethyl trifluoroacetate by hydrazinolysis, cyclization of phosphorus oxychloride, nucleophilic substitution of ethylenediamine and closed-loop reaction. The process has the advantages of high yield, mild reaction conditions, simple operation and simple solvent recovery.
Keywords:3-(trifluoromethyl)-5  6  7  8-tetrahydro [1  2  4] triazole [4  3-α] piperazine hydrochloride  Sitagliptin side chain piperazine hydrochloride  Process optimization
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