Palladium-Catalyzed Enantioselective Relay Heck Arylation of Enelactams: Accessing αβ-Unsaturated δ-Lactams

摘要

In this report, we describe the construction of chiral α,β-unsaturated δ-lactams, a widely used pharmacophore, in high yields and excellent enantioselectivities using an oxidative relay Heck arylation reaction. This strategy also allows facile access to 7-substituted α,β-unsaturated ε-lactam products and δ-lactams containing a tetrasubstituted nitrogen-bearing stereocenter.