非肽类蛋白酶抑制剂甲磺酸卡莫司他的合成

Synthesis of Camostat Mesilate as a Nonpeptidic Protease Inhibitor

合成甲磺酸卡莫司他。将对胍基苯甲酸盐酸盐制备为酰氯,与对羟基苯乙酸-N,N-二甲基甲酰氨基甲酰甲酯在催化剂吡啶作用下制备甲磺酸卡莫司他,总收率为57.1%。获得高纯度的甲磺酸卡莫司他,本工艺适合工业化生产。

Camostat mesilate was synthesyzed from p -guanidinobenzoic acid hydrochloride and N,N -dimethylcarbamoylmethyl-p-hydroxyphenylacetate using pyridine as catalysts. The total yield was 57.1% withhigh purity. The process is industrially applicable.