铜（I）催化的吲哚与 2-芳基-N-磺酰基氮丙啶作为烷基化试剂的对映选择性弗里德尔-克拉夫茨烷基化反应。
Cu(I)-Catalyzed Enantioselective Friedel-Crafts Alkylation of Indoles with 2-Aryl-N-sulfonylaziridines as Alkylating Agents.
机构信息
College of Chemical Engineering, Zhejiang University of Technology , Hangzhou 310014, China.
出版信息
Org Lett. 2016 Jul 1;18(13):3122-5. doi: 10.1021/acs.orglett.6b01317. Epub 2016 Jun 16.
PMID:27309541
Abstract
A highly enantioselective Friedel-Crafts alkylation of indoles with N-sulfonylaziridines as alkylating agents has been developed by utilizing the complex of Cu(CH3CN)4BF4/(S)-Segphos as a catalyst. A range of optically active tryptamine derivatives are obtained in good to excellent yields and enantioselectivities (up to >99% ee) via a kinetic resolution process.
摘要
一种高效对映选择性的 Friedel-Crafts 吲哚烷基化反应已经被开发出来，其中 N-磺酰基氮丙啶作为烷基化试剂，利用 Cu(CH3CN)4BF4/(S)-Segphos 配合物作为催化剂。通过动力学拆分过程，可以获得一系列光学活性色胺衍生物，产率和对映选择性都很好（高达>99%ee）。
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