Synthesis of P -Stereogenic Phosphinamides via Pd(II)-Catalyzed Enantioselective C-H Alkynylation.

P -Stereogenic phosphinamides represent important structural elements in chiral organocatalysts and bioactive compounds. Herein, we report Pd(II)-catalyzed enantioselective C-H alkynylation using cheap commercially available l-pyroglutamic acid as a chiral ligand. A range of structurally diverse P -stereogenic phosphinamides was prepared in good yields with high enantioselectivities via desymmetrization and kinetic resolution. A tailor-made congested directing group, N -ethyl- N -(3-methylpyridin-2-yl)amino, was crucial for the reactivity.