Palladium-catalyzed sequential monoarylation/amidation of C(sp 3 )-H bonds: stereoselective synthesis of α-amino-β-lactams and anti-α,β-diamino acid.

Pd-Catalyzed sequential monoarylation/amidation of C(sp ³ )-H bonds of alanine enabled by a removable 5-methoxyquinolin-8-amine (MQ) auxiliary is described. This process is highly efficient and compatible with a variety of functional groups, providing a general and practical access to various α-amino-β-lactams. The synthetic potential of this protocol is further demonstrated by the stereoselective synthesis of orthogonally protected anti-α,β-diamino acids.