Rhodium-catalyzed regioselective amidation of indoles with sulfonyl azides via C-H bond activation.Org Biomol Chem. 2012 Dec 07; 10(45):8953-5.OB
Direct C-2 amidation of indoles was reported using sulfonyl azides as the amino source to release N(2) as the single byproduct. This reaction exhibits high functional group tolerance and regioselectivity, providing a variety of 2-amino substituted indoles in high to excellent yield. The procedure is robust, reliable, and compatible with water and air.