A Copper-Catalyzed Synthesis of 3‑Aroylindoles via a sp<sup>3</sup> 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 <i>o</i>-alkynylated <i>N</i>,<i>N</i>-dimethylamines via a sp<sup>3</sup> C–H bond activation α to the nitrogen atom followed by an intramolecular nucleophilic attack with the alkyne using an aqueous solution of <i>tert</i>-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 sp<sup>3</sup> C–H bond cleavages.