广东化工
廣東化工
엄동화공
GUANGDONG CHEMICAL INDUSTRY
2012年
10期
29-30
,共2页
夏正君%马堰启%林送%陈再新
夏正君%馬堰啟%林送%陳再新
하정군%마언계%림송%진재신
阿托伐他汀钙非对映异构体%合成%杂质
阿託伐他汀鈣非對映異構體%閤成%雜質
아탁벌타정개비대영이구체%합성%잡질
(3S,5R)-epimers ofatorvastatin calcium%synthesis: impurities
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:合成得到了翻标化合物,可为阿托伐他汀钙的杂质研究提供可靠参数。
目的:閤成阿託伐他汀鈣非對映異構體。方法:以(R)-6-氰基-3-氧代-己痠叔丁酯為起始原料經羰基還原、O-烴化、氰基還原、與M-4髮生Paal.Knorr反應、脫保護、酯水解、成鹽等共7步反應閤成瞭阿託伐他汀鈣異構體(3S,5R)(1)。其結構經^1H—NMR、ESI—MS、HPLC確證。結論:閤成得到瞭翻標化閤物,可為阿託伐他汀鈣的雜質研究提供可靠參數。
목적:합성아탁벌타정개비대영이구체。방법:이(R)-6-청기-3-양대-기산숙정지위기시원료경탄기환원、O-경화、청기환원、여M-4발생Paal.Knorr반응、탈보호、지수해、성염등공7보반응합성료아탁벌타정개이구체(3S,5R)(1)。기결구경^1H—NMR、ESI—MS、HPLC학증。결론:합성득도료번표화합물,가위아탁벌타정개적잡질연구제공가고삼수。
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.