Highly Enantioselective Catalytic Addition of Grignard Reagents to N-Heterocyclic Acceptors

Abstract

General methods to prepare chiral N-heterocyclic molecular scaffolds are greatly sought after because of their significance in medicinal chemistry. Described here is the first general catalytic methodology to access a wide variety of chiral 2- and 4-substituted tetrahydro-quinolones, dihydro-4-pyridones, and piperidones with excellent yields and enantioselectivities, utilizing a single catalyst system.

Keywords: Grignard reagent; Michael addition; alkaloids; asymmetric catalysis; copper.