Enaminone-directed ruthenium(ii)-catalyzed C–H activation and annulation of arenes with diazonaphthoquinones for polycyclic benzocoumarins

Abstract

The weakly coordinating enaminone functionality has been leveraged for a C–H bond activation strategy under ruthenium catalysis and employed in the regioselective annulative coupling of arenes with diazonaphthoquinones, offering polycyclic benzocoumarins in very high yields. The enaminone motif plays a dual role and the protocol operates through a Ru(II)/Ru(IV) catalytic pathway which is amenable to the diversification of various pharmacophore-coupled substrates.