| 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。 |
| 关键词: 奥美沙坦酯 合成 优化 |
| DOI： |
| 分类号:R284.1；R917.101 |
| 基金项目: |
|
| Improvement of Process for Olmesartan Medoxomil |
|
WANG Peng1,2, ZENG Su1
|
|
1.College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China;2.Zhejiang Huahai Pharmaceutical Co., Ltd., Taizhou 317016, China
|
| 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. |
| Key words: olmesartan medoxomil synthesis optimization |
