An efficient Pd(OAc)2 catalyzed, Csp2-Csp bond formation through tautomerizable quinolinones by reacting with different alkynes furnished alkynyl quinolines in excellent yields. The C-OH bond activation is facilitated by using BOP reagent in the presence of Ruphos/THF/H2O system under copper-free aqueous conditions, which yields chemo-selectivity and could be a greater synthetic utility. © 2020 Taylor & Francis Group, LLC.