Direct Synthesis of 2-Aryl-4-quinolones via Transition-Metal-Free Intramolecular Oxidative C(sp3)-H/C(sp3)-H Coupling

A novel, metal-free oxidative intramolecular Mannich reaction was developed between secondary amines and unmodified ketones, affording a simple and direct access to a broad range of 2-arylquinolin-4(1H)-ones through C(sp(3))-H activation/C(sp(3))-C(sp(3)) bond formation from readily available N-arylmethyl-2-aminophenylketones, using TEMPO as the oxidant and (KOBu)-Bu-t as the base.