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

A general and user‐friendly synthesis of β‐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 enantioselective version using a chiral phosphonite ligand is demonstrated. Finally, this method can be employed to synthesize valuable enantiopure free β‐lactams and β‐amino acids.