摘要
目的对抗高血压药物阿齐沙坦的合成工艺进行研究,使之能工业化生产。方法以1-[(2'-氰基联苯-4-基)甲基]-2-乙氧基-1H-苯并咪唑-7-甲酸甲酯为起始原料,经缩合、成环、水解三步反应得到阿齐沙坦。结果中间体和目标化合物的结构经过质谱、核磁共振氢谱确证,总收率达到31%。结论新的合成路线操作简便,收率高,适合工业化生产。
Objective：To improve the synthetic procedure of Azilsartan. Method：Started from Methyl 1-[ （2 ＇-cyanobiphenyl-4-yl）methyl] -2-ethoxy-1H-benzimidazole-7-carboxylate, Azilsartan was synthesized by condensation, cyclization and hydrolysis. Results：The structure of intermediate and Azilsartan was confirmed by MS and 1H-NMR. The overall yield is 31%. Conclusion： The improved process has the advantage of easy operation, high yield and is suitable for industrial production.
出处
《化工时刊》
CAS
2015年第8期10-12,31,共4页
Chemical Industry Times
关键词
阿齐沙坦
合成
抗高血压
工艺改进
Azilsartan
synthesis
anti-hypertension
process improvement
