Synthesis of α,β-Unsaturated Amidines through Gold-Catalyzed Intermolecular Reaction of Azides with Ynamides.

A concise and flexible synthesis of alpha,beta-unsaturated amidines via gold-catalyzed intermolecular ynamide amination/carbene 1,2-shift between ynamides and benzylic azides has been developed. Under mild reaction conditions, various alpha,beta-unsaturated amidines were obtained in mostly good yields, thus providing an efficient and atom-economic way for the construction of valuable alpha,beta-unsaturated amidines.