One-Pot and Mild Synthesis of Novel Antibacterial 3-(1,3,4-Oxadiazol-2-yl)isoindolin-1-ones via On-Step Four-Component Dicyclization Reaction

A novel and efficient four-component dicyclization strategy has been developed for one-step constructing diverse antibacterial 3-(1,3,4-oxadiazol-2-yl)isoindolin-1-ones under very mild base-free and metal-free conditions without other additives. This one-pot process underwent two consecutive cyclization reactions including tandem Ugi/aza-Wittig reaction and N-acylation by utilizing (N-isocyanimine)triphenylphosphorane, methyl 2-formylbenzoate, primary amines, and carboxylic acids. The method was conferred its favorable characteristics, including ambient temperature conditions, one-step synthesis, without any additives, facile gram-scale synthesis, and good yields.