化工进展

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胰腺炎治疗药甲磺酸卡莫司他的合成工艺

陈宝泉,李彩文,史艳萍,麻 静,卢学磊   

  1. 天津理工大学化学化工学院
  • 出版日期:2010-07-05 发布日期:2010-07-05

Synthetic process for camostat mesilate——A drug for pancreatitis treatment

CHEN Baoquan,LI Caiwen,SHI Yanping,MA Jing,LU Xuelei   

  1. College of Chemistry and Chemical Engineering,Tianjin University of Technology
  • Online:2010-07-05 Published:2010-07-05

摘要: 研究了抗胰腺炎药甲磺酸卡莫司他的合成工艺,以对氨基苯甲酸和氰胺为原料,通过优化反应条件,合成了对胍基苯甲酸盐酸盐,它与对羟基苯乙酸-N,N-二甲基氨基甲酰甲酯在二环己基碳二亚胺(DCC)参与下,用4-二甲氨基吡啶(DMAP)作催化剂制备了目标产物,该方法操作简便,原料易得,易于工业化推广。

Abstract: Camostat mesilate,a drug for pancreatitis treatment was prepared from p-guanidinobenzoic acid hydrochloride and N,N-dimethylcarbamoylmethyl-p-hydroxyphenylacetate in the presence of DCC(N,N-dicyclohexylcarbodiimide)using DMAP(4-dimethylaminopyridine)as catalyst. p-Guanidinobenzoic acid hydrochloride was prepared from p-aminobenzoic acid and cyanamide by optimization of reaction conditions. This process is simple with easily available starting materials,which is suitable for industrial production.

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