埃索美拉唑钠不对称氧化合成工艺的研究进展

Asymmetric oxidation synthesis of esomeprazole sodium:research advances

埃索美拉唑钠是应用广泛的质子泵抑制剂,主要用于胃溃疡、十二指肠溃疡、消化性食管炎及胃炎的治疗。本文通过总结近10年有关埃索美拉唑钠不对称氧化合成的文献,归纳其合成的工艺流程,并从产率、立体选择性及后处理等方面着重比较不同催化体系下关键合成步骤,以期选择合适的手性催化剂来降低埃索美拉唑钠合成成本。结论为大部分合成工艺中所采用的催化剂负载量大、成本高。相较于经典的Kagan-Modena体系,Ti-salan催化剂在埃索美拉唑钠的合成上有一定的优势,可推广使用。

Esomeprazole sodium is a widely used proton pump inhibitor which is mainly applied to the treatment of gastric ulcer,duodenal ulcer,digestive esophagitis and gastritis.By reviewing the literature over the past decade on the asymmetric oxidation of esomeprazole sodium,the paper summarizes the synthetic process and focuses on the comparison of the critical steps.To choose suitable chiral catalyst to reduce the cost of synthesis of esomeprazole sodium,this paper compares beyond the yield,enantioselectivity and other aspects.The conclusion is that the catalysts used in the most of oxidation systems are with a large load and high cost,and compared with the classical Kagan-Modena system,the Ti-salan catalyst has advantages in the synthesis of esomeprazole sodium,and can be widely used.