Direct Synthesis of 3-Acylindoles through Rhodium(III)-Catalyzed Annulation of N-Phenylamidines with α-Cl Ketones

• DOI: 10.1021/acs.orglett.8b03383
• Publication Date: 2018-11-20T16:41:42Z
• Authors: Jianhui Zhou; Jian Li; Yazhou Li; Chenglin Wu; Guoxue He; Qiaolan Yang; Yu Zhou; Hong Liu
• Keywords: 01 natural sciences; 0104 chemical sciences

In the present study, a novel synthetic strategy to directly produce versatile 3-acylindoles through Rh(III)-catalyzed C-H activation and annulation cascade of N-phenylamidines with α-Cl ketones was developed, in which α-Cl ketones serve as unusual one-carbon (sp3) synthons. This strategy features high regioselectivity, efficiency, wide substrate tolerance, and mild reaction conditions, which further underscore its synthetic utility in drug molecule synthesis.