Synthesis of polysubstituted 1,2-dihydroisoquinolines via a CuI-catalyzed arylation/condensation cascade process

CuI-catalyzed reaction of 1-(2-bromophenyl)-propargylamines 4 with β-keto esters in i-PrOH/H2O (3:1) at 50 °C provides polysubstituted 1,2-dihydroisoquinolines. The transformation involves a cascade intermolecular C–C bond formation and intramolecular condensation process.