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.