培哚普利合成工艺的改进

Improved Synthesis of Perindopril

文章以(S)-2-((S)-1-乙氧基-1-氧戊丹-2-基氨基)丙酸为起始原料,经过甲酰化、酰胺、碱成盐、酸析后合成培多普利,最后与精氨酸成盐合成培多普利精氨酸。培多普利粗品合成和提纯采用一步合成工艺,未经过中间体提纯,反应大大缩减了操作步骤,合成过程中采用三光气作为甲酰化试剂,可有效合成环酰亚胺内脂,反应过程中原料用量少。该工艺路线原料成本低,工艺安全环保,制备的产品与同类产品相比品质佳、性能优异,市场需求量大,竞争力强。

In this paper,using(s)-2-((s)-1-ethoxy-1-oxopentane-2-ylamino)propionic acid as the starting material,pedopril was synthesized by formylation,amidation,alkali salting and acid analysis,and f inally was salted with arginine to synthesize pedopril arginine.The synthesis and purif ication of crude perindopril adopt one-step synthesis process without intermediate purif ication,which greatly reduces the operation steps.Triphosgene is used as formylation reagent in the synthesis process,which can effectively synthesize cycloimideendolipid with less raw materials.Compared with other similar products,the product has good quality,excellent performance,large market demand and strong competitiveness.