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.