Pd(II)-Catalyzed Tandem Enantioselective Methylene C(sp3)-H Alkenylation-Aza-Wacker Cyclization to Access β-Stereogenic γ-Lactams

Herein, we describe an unprecedented cascade reaction to beta-stereogenic gamma-lactams involving Pd(II)-catalyzed enantioselective aliphatic methylene C(sp(3))-H alkenylation-aza-Wacker cyclization through syn-aminopalladation. Readily available 3,3 '-substituted BINOLs are used as chiral ligands, providing the corresponding gamma-lactams with broad scope and high enantioselectivities (up to 98 % ee).