Journal of the American Chemical Society, Vol.140, No.21, 6527-6530, 2018
Palladium-Catalyzed Enantioselective Relay Heck Arylation of Enelactams: Accessing alpha,beta-Unsaturated delta-Lactams
In this Communication, we describe the construction of chiral alpha,beta-unsaturated delta-lactams, widely used as pharmacophores, in high yields and excellent enantioselectivities using an oxidative relay Heck arylation reaction. This strategy also allows facile access to 7-substituted alpha,beta-unsaturated epsilon-lactam products and delta-lactams containing a tetrasubstituted nitrogen-bearing stereocenter.