Rhodium-catalyzed regioselective C-H chlorination of 7-azaindoles using 1,2-dichloroethane
An unexpected rhodium-catalyzed regioselective C-H chlorination of 7-azaindoles was developed using 1,2-dichloroethane (DCE) as a chlorinating agent and 7-azaindole as the directing group. This protocol provides an efficient access to ortho-chlorinated azaindoles with operational simplicity, good functional group tolerance, and a wide substrate scope. (Chemical Equation Presented).
Qian, Guangyin,Hong, Xiaohu,Liu, Bingxin,Mao, Hong,Xu, Bin
Synthesis of 1-aryl-1H-pyrrolo[2,3-b]pyridines (1-aryl-7-azaindoles) by a thermal dehydration-cyclization-dehydrogenation sequence of 2-arylamino-3-(1- hydroxyalkyl)pyridines
1-Aryl-1H-pyrrolo[2,3-b]pyridines (1-aryl-7-azaindoles) have been prepared in reasonable yields from the corresponding 2-arylamino-3-(1-hydroxyalkyl) pyridines, on heating at ca. 250 °C, through a successive dehydration/cyclization/dehydrogenation sequenc