Chen Ping, Lu Sheng-mei, Guo Wengang, Liu Yan, Li Can
State Key Laboratory of Catalysis, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, P. R. China.
Chem Commun (Camb). 2016 Jan 4;52(1):96-9. doi: 10.1039/c5cc07721d.
A highly enantioselective approach for the synthesis of 3-alkyl- indole or indoline derivatives with a functional thiol group is presented. The chemistry is based on the asymmetric 1,4-addition of thiol to vinylogous imine intermediates, which are generated in situ from sulfonylindoles. The broad substrate transformation proceeds with high yields (up to 96%) and enantioselectivity (up to 98% ee) in a water-compatible system.
本文提出了一种用于合成具有功能性硫醇基团的3-烷基吲哚或二氢吲哚衍生物的高度对映选择性方法。该化学方法基于硫醇对烯醇式亚胺中间体的不对称1,4-加成反应，这些中间体由磺酰基吲哚原位生成。在与水兼容的体系中，广泛的底物转化反应以高产率（高达96%）和对映选择性（高达98% ee）进行。
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