Copper‐(II) Catalyzed N‐Formylation and N‐Acylation of Aromatic, Aliphatic, and Heterocyclic Amines and a Preventive Study in the C‐N Cross Coupling of Amines with Aryl Halides

Abstract

AbstractA Cu‐(II) catalyzed N‐formylation and N‐acylation of amines with moderate to excellent yields, using N, N‐dimethyl formamide (DMF) and N, N‐dimethyl acetamide (DMA) as a formyl and acylating sources in the presence of 1,2,4‐triazole is reported. This novel, highly efficient and simple protocol shows broad substrate scope for aliphatic, aromatic, and heterocyclic amines. In addition, the conditions to prevent N‐formylation and N‐acylation impurities in the C−N cross coupling of amines and aryl halides are described typically when DMF and DMA are used as solvents, with various catalysts, ligands, and bases.