Rhodium(III)-Catalyzed Addition of Indoles with Boc-Imines via C-H Bond Activation

A rhodium-catalyzed alkylation reaction of indoles with N-Boc-imines has been developed via C-H activation to afford a series of substituted 2-indolyl-methanamine derivatives with good functional group tolerance and regioselectivity. A wide range of indole-based alkylation products could be obtained in up to 95% yield.本研究开发了一种经由C-H活化（C-H activation）的铑催化吲哚（indoles）与N-叔丁氧羰基亚胺（N-Boc-imines）的烷基化反应，可得到一系列取代2-吲哚基甲胺衍生物，该反应具备良好的官能团耐受性与区域选择性。多种基于吲哚的烷基化产物的产率最高可达95%。