Synthesis of β-Lactams by Palladium(0)-Catalyzed C(sp3)−H Carbamoylation

A general and user-friendly synthesis of beta-lactams is reported that makes use of Pd-0-catalyzed carbamoylation of C(sp(3))-H bonds, and operates under stoichiometric carbon monoxide in a two-chamber reactor. This reaction is compatible with a range of primary, secondary and activated tertiary C-H bonds, in contrast to previous methods based on C(sp(3))-H activation. In addition, the feasibility of an enantio-selective version using a chiral phosphonite ligand is demonstrated. Finally, this method can be employed to synthesize valuable enantiopure free beta-lactams and beta-amino acids.