甲磺酸卡莫司他关键中间体的合成

Synthesis of Key Intermediate of Camostat Mesilate

以对胍基苯甲酸盐酸盐和对羟基苯乙酸-N,N-二甲基甲酰氨基甲酰甲酯为原料、草酰氯为卤化剂、吡啶为缚酸剂合成了甲磺酸卡莫司他关键中间体N,N-二甲基氨基甲酰甲基-4-(4-胍基苯甲酰氧基)苯乙酸酯盐酸盐,总收率96.6%,并优化了其合成工艺。产物结构经1 HNMR、13 CNMR和质谱确证。该合成方法原料易得,反应条件温和,适合工业化生产。

Using p-guanidinobenzoic acid hydrochloride and p-hydroxyphenylacetic acid-N,N-dimethylformamide formyl methyl ester as raw materials,oxalyl chloride as a halogenating agent,pyridine as a acid acceptor,the key intermediate of camostat mesilate[N,N-dimethylcarbamoylmethyl-4-（4-guanidinobenzoyloxy）phenylacetate hydrochloride]was synthesized with the total yield of 96.6%.And the synthetic process was optimized.The structure of target compound was confirmed by 1HNMR,13 CNMR and MS.This method has advantages of ease to obtain raw materials,mild reaction conditions,and suitable for industrial productions.