Palladium Catalysis Enabled Sequential C(sp 3 )-H/C-C Activation: Access to Vinyl γ-Lactams.

A Pd(II)-catalyzed tandem reaction of aliphatic amides with vinylcyclopropanes (VCPs) was accomplished by merging C(sp 3 )-H and C-C activation. The reaction of VCP revealed alkenylation/cyclization, followed by ring opening via C-C cleavage, delivering vinyl γ-lactams with ( E )-selectivity. The role of ligands, site-selectivity, functional group diversity, mechanistic insight, and synthetic utilities are important practical features.