Ligand Accelerated Site-Selective Csp2–H and Csp3–H Alkynylation of Alcohols via Pd(II) Catalysis

A ligand accelerated site-selective C–H alkynylation of weak coordinated while synthetic promising alcohols, via putative 6, 7 and 8-membered palladacycle intermediates, was developed. In contrast to well-developed endo-type C–H activation of olefins, we developed herein an exo C‒H alkynylation of alkenols. Significantly, by judicious choice of amide attached oximes, challenging secondary and tertiary Csp3‒H alkynylation of alcohols, were also realized.