Synthetic studies on statins. Part 1: a short and cyanide-free synthesis of atorvastatin calcium via an enantioselective aldol strategy

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• 作者：Lemeng Hu ; Fangjun Xiong ; Xiaofei Chen ; Wenxue Chen ; Qiuqin He ; ^{qqhe@fudan.edu.cn} ; Fener Chen ; ^{rfchen@fudan.edu.cn}
• 刊名：Tetrahedron: Asymmetry
• 出版年：2013
• 出版时间：28 February, 2013
• 年：2013
• 卷：24
• 期：4
• 页码：207-211
• 全文大小：543 K

文摘

A short and cyanide-free enantioselective synthesis of atorvastatin calcium has been achieved starting from a commercially available highly substituted 1,4-diketone in an overall yield of 40 % . The key step in this approach is the asymmetric aldol reaction of an aldehyde with diketene in the presence of Ti(O-i-Pr)₄-Schiff base complex to create the (5R)-stereochemistry of atorvastatin calcium.