文献类型：期刊文献

中文题名：氯吡格雷硫酸氢盐合成工艺改进

英文题名：Improved Synthesis of Clopidogrel Hydrogen Sulfate

作者：林治秘[1];张兰英[1];吴范宏[2];赵敏[2];陈建中[2]

机构：[1]山东省医药工业研究所,济南250100;[2]华东理工大学化学与分子工程学院,上海200237

年份：2010

卷号：12

期号：7

起止页码：235

中文期刊名：食品与药品

外文期刊名：Food and Drug

收录：CSTPCD

语种：中文

中文关键词：氯吡格雷;工艺改进;拆分

外文关键词：clopidogrel;process improvement;resolution

摘要：目的改进硫酸氢氯吡格雷的合成工艺。方法研究了邻氯苯甘氨酸甲酯的合成及拆分,2-氯苯基-2-噻吩乙胺基乙酸甲酯盐酸盐合成新方法,氯吡格雷硫酸氢盐的合成改进等。结果大范围改进了现有氯吡格雷制备工艺,工艺总收率52.5%。结论该工艺操作简便,稳定性好,收率高,适用于工业化生产。
Objective To improve the synthesis of clopidogrel hydrogen sulfate.Methods The synthesis and resolution of o-chlorophenyl glycine methyl ester,a new synthetic method of 2-chlorophenyl-2-thienylethamino methyl acetate hydrochloride and an improved synthesis of clopidogrel hydrogen sulfate were researched.Results The existing preparation process of clopidogrel was modif ied greatly and the total yield of the whole process reached 52.5%.Conclusion This improved process is simple,stable,productive and suitable for the industrial production.