Synthesis of P‑Stereogenic Benzoazaphosphole 1‑Oxides via Alkynylation of P‑Stereogenic ortho-Aurated and ortho-Iodo Phosphinic Amides

An efficient methodology for the synthesis of P-stereogenic dihydrobenzoazaphosphole 1-oxides via intramolecular 5-exo-dig alkyne hydroamination promoted by tetrabutylammonium fluoride is herein described. The required chiral o-alkynylphosphinic amide starting materials were prepared in high yields under very mild reaction conditions through alkynylation of P-stereogenic (O^C)-cyclometalated (phosphinic amide)­dichlorogold­(III) complexes and Sonogashira cross-coupling of ortho-iodo P-stereogenic phosphinic amide.