Regioselective assembly of 3,4-dihydroisoquinoline derivatives

Abstract A facile two-step sequence ( 9 → 10 → 1 ) of regioselective assembly of 3,4-dihydroisoquinoline derivatives 1 is reported. The halogen derivatives provide opportunity for Suzuki, Buchwald, and related coupling reactions useful for expanding the scaffold and lead optimization in drug discovery.