Synthesis of 2-Benzyl-3-(2-oxo-2-phenylethyl)isoindolin-1-one Derivatives in Water under Catalyst-Free Conditions

Abstract We have developed a catalyst-free synthesis of a series of isoindolinone derivatives via a one-pot, three-component reaction in water using o-formylbenzoic acids, primary amines, and acetophenones as starting materials. An investigation of the influence of the solvent, the substrate molar ratio, the temperature, and the reaction time revealed that the reaction proceeded optimally in water at 70 °C over 12 hours to afford a wide range of isoindolinone derivatives in yields of up to 93%. This method has the advantages of mild reaction conditions, environmental friendliness, and a broad substrate scope.