阿托伐他汀钙非对映异构体(3S,5R)的全合成

Total Synthesis of (3S,5R)- epimers of Atorvastatin Calcium

目的:合成阿托伐他汀钙非对映异构体。方法:以(R)-6-氰基-3-氧代-己酸叔丁酯为起始原料经羰基还原、O-烃化、氰基还原、与M-4发生Paal-Knorr反应、脱保护、酯水解、成盐等共7步反应合成了阿托伐他汀钙异构体(3S,5R)(1)。其结构经1H-NMR、ESI-MS、HPLC确证。结论:合成得到了目标化合物,可为阿托伐他汀钙的杂质研究提供可靠参数。

Objective： To synthesis （3S, 5R）-epimers of Atorvastatin Calcium. Methods： The （3S, 5R）-epimers of Atorvastatin Calcium was obtained from （R）-tert-butyl 6-cyano- 5-hydroxy -3-oxohexanoate by condensation of carbonyl group, O-alkylation, condensation of cyanogroup, Paal-Knorr reaction with M-4, deprotection, hydrolysis of ester, salinization. The structures were confin-aed by ^1H-NMR, ESI-MS, HPLC. Conclusion： The target compound was synthesized by this method, which provides an important reference for the research on impurities of atorvastatin.