A Copper-Catalyzed Synthesis of 3‑Aroylindoles via a sp³ C–H Bond Activation Followed by C–C and C–O Bond Formation

An efficient Cu(I)-catalyzed synthesis of 3-aroylindoles has been achieved from o-alkynylated N,N-dimethylamines via a sp³ C–H bond activation α to the nitrogen atom followed by an intramolecular nucleophilic attack with the alkyne using an aqueous solution of tert-butyl hydroperoxide (TBHP) as the oxidant. In this tandem catalytic synthesis of 3-aroylindoles both C–C and C–O bonds are installed at the expense of two sp³ C–H bond cleavages.