Highly Efficient and Eco‐Benign Synthesis of 3‐Imidazoheterocyclic‐Substituted Phthalides/Isoindolinones in Water under Catalyst‐ and Additive‐Free Conditions

A novel catalyst‐ and additive‐free method for synthesis of structurally diverse 3‐imidazoheterocyclic‐substituted phthalides/isoindolinones has been developed in water with good to excellent yields via cyclization reactions of imidazoheterocycles with phthalaldehydic acid and amine. The broad substrate scope, good functional group tolerance, high atom economy, and environmentally benign quality of this method make it an attractive alternative for synthesis of complex biheterocyclic compounds, which are privileged structures in many biologically active compounds.