One‐Step and Mild Synthesis of Antibacterial 3‐(1,3,4‐Oxadiazol‐2‐yl)isoindolin‐1‐ones via Ugi Four‐Component Domino Dicyclization

A novel and efficient Ugi four‐component domino dicyclization strategy has been developed for one‐step constructing diverse 3‐(1,3,4‐oxadiazol‐2‐yl)isoindolin‐1‐ones in good yields under without other additives. This domino dicyclization process underwent three consecutive reactions including Ugi, aza‐Wittig and N‐acylation by utilizing (N‐isocyanimine)triphenylphosphorane, methyl 2‐formylbenzoate, primary amines, and carboxylic acids. The initial biological activity testing revealed that compound 5i exhibited good antibacterial activity against certain fungi and demonstrated versatile applications in the fields of synthesis and pesticide chemistry.