Synthesis ofP-Stereogenic Phosphinamides via Pd(II)-Catalyzed Enantioselective C–H Alkynylation

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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.