Process optimization on the synthesis of atorvastatin calcium
Zhengjun Xia · 2012
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-1,3dioxan4-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.