【摘要】 目的合成血管紧张素Ⅱ受体拮抗剂替米沙坦。方法以3-甲基-4-硝基苯甲酸为起始原料,经酯化、还原、丁酰化、硝化、还原、环合、水解得2-正丙基-4-甲基-6-羧基苯并咪唑,在多聚磷酸的作用下与N-甲基邻苯二胺缩合,生成的产物再与4′-溴甲基联苯-2-甲酸甲酯缩合、水解得替米沙坦。结果目标物收率从文献的20·9%提高到26·3%。结论与文献相比,该合成工艺具有原料易得、操作简便、收率较高、易于工业化生产等优点。更多还原

【Abstract】 Aim To synthesize telmisartan,an angiotensin Ⅱ receptor antagonist. Method The target compound was synthesized from 3-methyl-4-nitrobenzoic acid via esterification,reduction,butyrylation,nitration,reduction,cyclization and hydrolysis to give 2-n-propyl-4-methyl-6-carboxybenzimidazole,which was condensed with N-methyl-o-phenylenediamine and followed by condensation with 4′-bromomethyl-biphenyl-2-carboxylic acid methyl ester. Result The yield is increased from 20.9% to 26.3%. Conclusion In comparison with the method reported,the method is with the advantages of high yield,simple procedure and low cost.更多还原