Pd-Mediated γ‑C(sp3)–H Bond Activation in Ammonia–Ugi 4‑CR Adducts by Using Picolinamide as Directing Group

The development of a novel protocol for the fast introduction of the picolinamide directing group in aliphatic ketones by using the ammonia–Ugi 4-CR reaction and the subsequent evaluation of the Pd-mediated γ-C­(sp3)–H bond activation is described. The methodology allows the efficient construction of a series of γ-arylated α-aminoamides bearing a congested carbon in two steps.