Rhodium-catalyzed regioselective amidation of indoles with sulfonyl azides via C-H bond activation.
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.
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China.
Jingjing
J
Shi
Bing
B
Zhou
Yaxi
Y
Yang
Yuanchao
Y
Li
D000577:Amides / Q000737:chemistry*; D001386:Azides / Q000737:chemistry*; D002244:Carbon / Q000737:chemistry*; D002384:Catalysis; D006859:Hydrogen / Q000737:chemistry*; D007211:Indoles / Q000737:chemistry*; D012238:Rhodium / Q000737:chemistry*; D013237:Stereoisomerism; D013379:Substrate Specificity
D000577:Amides; D001386:Azides; D007211:Indoles; D002244:Carbon; D006859:Hydrogen; D012238:Rhodium