An unprecedented Pd-catalyzed highly stereoselective synthetic strategy for the construction of a broad spectrum of polycyclic fused indoline skeletons employing N-halobenzoyl o-haloanilines and N-(prop-2-yn-1-yl)anilines as the substrates in the presence of Pd(PPh3)4 (10 mol%), Cu2O (20 mol %), BINOL-based phosphoramidite L (12 mol %), and K2CO3 (2.0 equiv) in 1,2-dichloroethane at 110 °C for 19 h under an argon atmosphere has been described. This Palladium-catalyzed protocol, which proceeds through a sequential intramolecular dearomative Heck annulation/phenyl electrophilic addition/dehydrogenation sequences, provides a straightforward, powerful, and atom-economical approach for accessing elaborated indoline quinoline derivatives in moderate-to-good yields.

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