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目的:合成阿托伐他汀内酯及酰胺产物。方法:以阿托伐他汀缩合物(3)为原料,经酸脱保护基,碱性条件酯水解得阿托伐他汀内酯5,化合物5与侧链(4R,6R)-6-(2氨-乙基)-2,2二-甲基-1,3二-氧六环-4乙-酸叔丁酯(2)反应得到中间体6,中间体6再经酸脱保护基,碱性条件酯水解,继而得到阿托伐他汀酰胺钙(1)。结果:其结构经1H-NMR和ESI-MS确证。结论:合成得到了目标化合物,可为阿托伐他汀的杂质研究提供可靠参数。
Objective: To synthesize atorvastatin lactone and amide product. Methods: Atorvastatin lactone 5 was synthesized from the atorvastatin condensate (3) via deprotection of the acid and hydrolysis with basic conditions. Compound 5 reacted with side chain (4R, 6R) -6- (2 Amino-ethyl) -2,2-di-methyl-1,3-dioxan-4-ylidene tert-butyl ester (2) to give intermediate 6 which was deprotected by acid followed by base Ester hydrolysis followed by atorvastatin calcium amide (1). Results: The structure was confirmed by 1H-NMR and ESI-MS. Conclusion: The target compounds were synthesized and could provide reliable parameters for the study of atorvastatin impurities.