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

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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… Click to show full 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.

Keywords: external auxiliary; reaction; primary amide; auxiliary free; hetero arylamides

Journal Title: Chemical communications
Year Published: 2022

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