替米沙坦的合成工艺改进

Improved Synthesis of Telmisartan

以 3 -甲基 -4 -氨基苯甲酸甲酯为起始原料 ,经酰化、硝化、还原、环合、水解得 4-甲基 -2 -正丙基 -6-甲氧羰基苯并咪唑 ,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 ,总收率为 15 .7%。

Telmisartan was synthesized from methyl 3 methyl 4 aminobenzoate via butyrylation, nitration, reduction, cyclization and hydrolysis to give 2 n propyl 4 methyl 6 methoxycarbonyl benzimidazole, which condensed with N methyl o phenylenediamine and followed by condensation with methyl 4′ bromomethyl biphenyl 2 carboxylic acid methyl ester. Telmisartan was obtained from hydrolysis of the latter in an overall yield of 15.7%.