Weak coordinated nitrogen functionality enabled regioselective C-H alkynylation via Pd(II)/mono-N-protected amino acid catalysis.

The exploration of weak coordinated amine derivative enabled regioselective C-H functionalization remains challenging due to the elusive achievement of reactivity and selectivity simultaneously. Herein, regioselective C-H alkynylation of various readily transformable nitrogen functionalities was developed with great efficiency, with the assistance of the mono-N-protected amino acid (MPAA) ligand via Pd(ii) catalysis proceeding via 5, 6 and 7-membered palladacycle intermediates.