Ru(ii)-catalyzed external auxiliary-free primary amide-directed inverse Sonogashira reaction on (hetero)arylamides

Abstract

Herein, we report ruthenium(II)-catalyzed weakly coordinating primary amide-assisted ortho-di-alkynylation of (hetero)arylamides via double C–H bond activation in the presence of bromo-alkynes as coupling partners. The attractive features of the developed strategy lie in the usage of an inexpensive ruthenium(II)-salt, external auxiliary-free directing group and simple reaction conditions, along with a broad substrate scope, high reaction yields and scale-up synthesis.