奥美沙坦酯的工艺改进

Improvement of Process for Olmesartan Medoxomil

摘要: 目的改进奥美沙坦酯的合成工艺。方法以2-氰基-4'-甲基联苯( 2 )为起始原料，经溴代反应，“一锅法”完成N-烷基化和皂化-酯化反应，再经氰基四氮唑化反应，得到奥美沙坦酯( 1 )。结果 3步得到成品，总收率46.5%(以2-氰基-4'-甲基联苯计)。结论改进后的工艺非常实用，适合工业化生产。

Abstract: OBJECTIVE To improve the synthesis process for olmesartan medoxomil. METHODS Olemsartan medoxomil( 1 ) was synthesized using 2-cyano-4'-methylbiphenyl( 2 ) as the starting material, via bromination, “one-pot” tandem N-alkylation/saponification-esterification sequence and tetrazolium reaction. RESULTS The total yield was 46.5% basing on the starting material 2-cyano-4'-methylbiphenyl over 3 steps. CONCLUSION The improved process is practical and suitable for industrial scaling-up.