Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, Fujian 361005, PR China.
Org Lett. 2012 Sep 21;14(18):4834-7. doi: 10.1021/ol302165d. Epub 2012 Aug 31.
A formal enantioselective total synthesis of the potent immunosuppressant FR901483 (1) has been accomplished. Our approach features the use of chiron 6 as the starting material, the application of the one-pot amide reductive bisalkylation method to construct the chiral aza-quaternary center (dr = 9:1), regio- and diastereoselective intramolecular aldol reaction to build the bridged ring, and ring closing metathesis to form the 3-pyrrolin-2-one ring.
已完成强效免疫抑制剂 FR901483（1）的正式对映选择性全合成。我们的方法以手性中心 6 为起始原料，采用一锅酰胺还原双烷基化方法构建手性氮杂季碳中心（dr = 9:1），区域和非对映选择性的分子内羟醛反应构建桥环，以及闭环复分解反应形成 3-吡咯啉-2-酮环。
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