Streamlined Catalytic Asymmetric Synthesis of Atorvastatin
Streamlined Catalytic Asymmetric Synthesis of Atorvastatin
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DOI：
10.1002/chem.201204609
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发表时间：
2013-03-01
影响因子：
4.3
通讯作者：
Shibasaki, Masakatsu
中科院分区：
文献类型：
--
作者：
Kawato, Yuji;Chaudhary, Sandeep;Shibasaki, Masakatsu
以直接催化不对称醛醇反应为基础，建立了一种高效的对映选择性合成阿托伐他汀的途径。初始醛醇反应中使用的昂贵的手性配体很容易回收（91%）并重复使用。采用氧-迈克尔反应构建syn - 1,3 -二醇装置，消除了几个多余的步骤，允许在六个步骤中快速获得常见中间体（见方案）。
An efficient enantioselective synthetic route to atorvastatin was developed based on a direct catalytic asymmetric aldol reaction. The expensive chiral ligand used in the initial aldol reaction was readily recovered (91%) and reused. Implementation of an oxy‐Michael reaction for the construction of the syn‐1, 3‐diol unit eliminated several redundant steps, allowing for rapid access to the common intermediate in six steps (see scheme).