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盐酸莫雷西嗪的合成
引用本文:王绍杰,郝东,陈欣,杨卓.盐酸莫雷西嗪的合成[J].中国新药杂志,2006,15(14):1188-1190.
作者姓名:王绍杰  郝东  陈欣  杨卓
作者单位:沈阳药科大学制药工程学院,沈阳,110016
摘    要:目的:合成抗心律失常药盐酸莫雷西嗪。方法:以3-溴硝基苯、乙酰苯胺为原料经烃化、水解反应得3-硝基二苯胺,经硫化亚铁-氯化铵-甲醇-水体系还原得3-氨基二苯胺,再经酰化、环合、烃化和成盐反应得盐酸莫雷西嗪。结果:合成了盐酸莫雷西嗪,9步反应总收率为35.8%。目标产物的结构经核磁共振氢谱、质谱确证。结论:本合成方法原料易得,操作简单,收率较高,适合大规模制备。

关 键 词:盐酸莫雷西嗪  药物合成  抗心律失常
文章编号:1003-3734(2006)14-1188-03
修稿时间:2005-12-23

Synthesis of moracizine hydrochloride
WANG Shao-jie,HAO Dong,CHEN Xin,YANG Zhuo.Synthesis of moracizine hydrochloride[J].Chinese Journal of New Drugs,2006,15(14):1188-1190.
Authors:WANG Shao-jie  HAO Dong  CHEN Xin  YANG Zhuo
Institution:College of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016,China
Abstract:Objective:To synthesize antiarrythmic drug moracizine hydrochloride.Methods: Starting from 3-bromonitrobenzene and acetanilide,the intermediate 3-nitrodiphenylamine was obtained via alkylation and hydrolysis.Subsequently,the target compound was synthesized via several chemical re- actions including reduction,acylation,cyclization,alkylation and saltization.Results:The total yield of moracizine hydrochloride was 35.8%,and the structure was verified by ~1H-NMR and MS.Conclusion:An easily manipulated synthetic procedure of moracizine hydrochloride was achieved for further pilot manufacture.
Keywords:moracizine hydrochloride  synthesis  antiarrythmia
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