坎地沙坦酯的合成工艺研究

Synthesis of candesartan cilexetil

目的合成抗高血压药坎地沙坦的前药坎地沙坦酯。方法以3-硝基邻苯二甲酸为起始原料,经酯化、重排、取代、水解、成酯、脱保护、精制合成高纯度的坎地沙坦酯。结果坎地沙坦酯总收率为35%。结论优化了合成路线,提高了收率,降低了成本,且节能环保。

Objective To synthesize candesartan cilexitil for high blood pressure. Methods A novel and practical synthetic route for preparation of candesartan cilexetil from 3-Nitro-phthalic acid was described. The key steps mainly included esterifi cation, rearrangement, substitution, hydrolysis, condensation and deprotection. Results The overall yield of this method was 35%. Conclusion Good synthetic route, excellent yield, lower cost and less pollution to the environment advantages of this method.