Oxidative C-H/N-H Annulation of Aromatic Amides with Dialkyl Malonates: Access to Isoindolinones and Dihydrobenzoindoles.

A copper-mediated oxidative C-H/N-H annulation of aromatic amides with dialkyl malonates has been presented to afford synthetically valuable dihydrobenzoindoles and isoindolinones. The reaction proceeds through direct oxidative C(sp(2))-H/C(sp(3))-H coupling followed by an intramolecular N-H/C(sp(3))-H dehydrogenative coupling to deliver the target motifs with broad scope and functional group tolerance.