Copper-Catalyzed Hydroxyl-Directed Aminoarylation of Alkynes

A facile, copper-catalyzed aminoarylation reaction of various aryl/alkyl alkynes was realized by utilizing N-fluoroarylsulfonimides (NFSI) as aminoarylation or amination reagent with hydroxyl as directing group. With this methodology, various α,β-unsaturated carbonyl compounds and indenones were efficiently constructed, and the synthetic application for indole derivatives was also provided. The aminoarylation reactions operate via a regiospecific addition of copper-coordinated nitrogen radical to C–C triple bond/Cvinyl–Caryl bond formation followed by other series of radical processes.