One‐Pot Multicomponent Synthesis of β‐Lactams via In Situ Generated Imines

Abstract An efficient, atom‐economic, multi‐component reaction protocol has been developed for the synthesis of β ‐lactams. This new procedure employs a one‐pot sequential multicomponent Staudinger reaction between acetic acid derivatives and imines generated in situ by thermal melting of an aryl or heteroaryl aldehyde with the primary amine. The protocol has the merits of simple operation, short reaction time, convenient work‐up, good yields, applicability to a broad range of substrates, cheap and less hazardousness to humans and environment. The structures of the β ‐lactam adducts E1‐30 were characterized by spectral (FT‐IR, 1 H‐NMR, 13 C‐NMR, GC‐MS) and elemental analyses.