Direct Regioselective Hydro(hetero)arylation/Cyclocondensation Reactions of -(2-Aminophenyl)-, -ynones by Means of Transition- Metal Catalysis/Bronsted Acid Synergism: Experimental Results and Computational Insights

Experimental results and computational insights explain the key role of transition-metal catalysis/Bronsted acid synergism in the achievement of the sequential regioselective direct heteroarylation/ cyclocondensation reactions of beta-(2-aminophenyl)-alpha,beta-ynones with a variety of electron-rich aromatic heterocyclic/arenes to afford quinoline-(hetero)aromatic hybrids. The first approach to the synthesis of 4-(1H-pyrrol-2-yl)quinolines is described. The effectiveness of various transition metals is compared.