关键词: 阿托伐他汀钙, 合成, 关键工艺, 优化

Abstract: The property and pharmacological actions of atorvastatin calcium were introduced briefly. The synthesis route of atorvastatin calcium was analyzed. The (4R-Cis)-6-{2-[2-(4-Fluoro phenyl)]-5-(isopro)-3-phenyl-4-[(phenylaminocarbonyl-1H-pyrrol-1-yl)ethyl]-2,2-dimethyl-1,3dioxan-4-tert-butyl acetate was selected as the raw material for the acidification and neutralization of Atorvastatin Calcium, and corresponding synthetic process was optimized. The total yield was 91.29% on the condition of 2 mol/L hydrochloric acid, 1∶2.2 molar ratio of material and hydrochloric acid, reaction time 75 min. Crude product was re-crystallized with n-hexane and dichloromethane, and formless atorvastatin Calcium was obtained. The structure characterization confirmed that the product was atorvastatin calcium.

Key words: atorvastatin calcium, synthesis, critical technology, optimization