Asymmetric Synthesis of the HMG-CoA Reductase Inhibitor Atorvastatin Calcium: An Organocatalytic Anhydride Desymmetrization and Cyanide-Free Side Chain Elongation Approach

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• 作者：Xiaofei Chen ; Fangjun Xiong ; Wenxue Chen ; Qiuqin He ; Fener Chen
• 刊名：Journal of Organic Chemistry
• 出版年：2014
• 出版时间：March 21, 2014
• 年：2014
• 卷：79
• 期：6
• 页码：2723-2728
• 全文大小：324K
• 年卷期：v.79,no.6(March 21, 2014)
• ISSN：1520-6904

文摘

An efficient asymmetric synthesis of atorvastatin calcium has been achieved from commercially available diethyl 3-hydroxyglutarate through a novel approach that involves an organocatalytic enantioselective cyclic anhydride desymmetrization to establish C(3) stereogenicity and cyanide-free assembly of C₇ amino type side chain via C₅+C₂ strategy as the key transformations.