Enantioselective Synthesis of Functionalized Tetrahydropyridines through Iridium-Catalyzed Formal [5+1] Annulation

An efficient iridium-catalyzed asymmetric formal [5+1] annulation by in situ generation of enamines as N-nucleophiles for the synthesis of tetrahydropyridine derivatives is disclosed. The methodology offers direct access to a wide variety of chiral tetrahydropyridine derivatives in moderate to good yields and excellent enantioselectivity.