| 摘要 |
The present invention provides an improved and commercially viable process for preparation of eprosartan and its pharmaceutically acceptable acid addition salts thereof in high purity and in high yield. Thus, for example, methyl 4-[[2-butyl-5-formyl-1 H-imidazol-1-yl]methyl]benzoate is reacted with ethyl 2-carboxy-3-(2-thienyl)propionate in the presence of a base, such as piperidine or piperidinium propionate in propionic acid, in cyclohexane solvent to give ethyl (αE)-α-[(2-n-butyl-1-[(4-(methoxy-carbonyl) phenyl]methyl]-1 H-imidazol-5-yl]methylene-2-thiophene propionate substantially free of decarboxylate impurity namely, ethyl 3-(2-thienyl)propionate, which is then subjected to base hydrolysis followed by treatment with methanesulfonic acid to obtain eprosartan mesylate in high purity and in high yield.
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