Scalable and Catalytic Asymmetric Synthesis of Atorvastatin from Chiral β-lactone

A catalytic asymmetric synthesis of atorvastatin is reported.Key to the success of this synthetic pathway including cinchona alkaloid-catalyzed acid chloride-aldehyde cyclocondensation (AAC) reaction to construct chiral β-lactone, followed by efficient construct 1,3-syn diol through Claisen condensation and Narasaka-Prasad reduction. Subsequent Fukuyama amine synthesis and pyrrole ring formation complete the total synthesis of atorvastatin.