Deoxygenative Alkynylation of Amides via C=O Bond Cleavage

A novel deoxygenative alkynylation of amides promoted by a synergistic action of a divalent rare-earth element and a transition metal has been developed. In this method, α-alkynyl substituted amines are synthesized from unactivated amides and alkynes in a single transformation. Broad substrate scope and excellent selectivity for CO cleavage has been demonstrated. This approach represents a general method for the construction of versatile α-alkynyl substituted amines from unactivated amide bonds.