Weak Coordinated Nitrogen Functionality Enabled Regioselective C-H Alkynylation via Pd(II)/Mono-Protected Amino Acid Catalysis

The exploration of synthetic versatile, while weak coordinated amine derivatives enabled regioselective C‒H functionaliza-tion, remained challenging due to the elusive achievement of reactivity and selectivity simultaneously. Herein, with the assis-tance of mono-protected amino acid (MPAA) ligand under Pd(II) catalysis, regioselective C-H alkynylation of various readi-ly transformable nitrogen functionality, was developed with great efficiency, which might proceed via 5, 6 and 7-membered palladacycle intermediates.