SYNTHETIC PROCESS OF ATORVASTATIN

摘要

A synthetic process of atorvastatin is provided to reduce reaction time and improve safety and yield of synthesis by inhibiting side reactions, performing reaction under mild temperature, and removing water generated in reactions with water-removing agent. A synthetic process of atorvastatin represented by the formula(1) comprises the steps of: condensation-reacting compound represented by the formula(2) in which R is methyl or ethyl with compound represented by the formula(3) in acid and alcohol solvent in the presence of water-removing agent at constant temperature to prepare compound represented by the formula(4); substituting an ester group of the compound represented by the formula(4) by aniline to prepare compound represented by the formula(5); and deprotecting the compound represented by the formula(5) and performing the calcium salt reaction, wherein the reaction temperature is 50-90°C. Further, the deprotecting reaction additionally comprises a hydrolysis reaction.