Oxidative C-H/N-H Annulation of Aromatic Amides with Dialkyl Malonates: Access to Isoindolinones and Dihydrobenzoindoles.
Sourav PradhanSubhasish RoySonbidya BanerjeePinaki Bhusan DeTharmalingam PunniyamurthyPublished in: The Journal of organic chemistry (2020)
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(sp2)-H/C(sp3)-H coupling followed by an intramolecular N-H/C(sp3)-H dehydrogenative coupling to deliver the target motifs with broad scope and functional group tolerance.