Abstract:

A solvent-free grinding reaction for the synthesis of 3-substituted isoindolin-1-ones from 2-cyanoarylaldehydes and various activated methylene compounds (such as dimethyl malonate and ethyl acetoacetate) has been developed. All the products were obtained without the tedious column chromatographic purification and were characterized using NMR spectroscopy and mass spectrometry. This method is advantageous because of its simple manipulation, short reaction time, wide substrate scope, high product yield, and high atom economy. It also has potential uses in novel-drug designing and natural product synthesis.

Key words: 2-Cyanoarylaldehyde, Activated methylene compound, 3-Substituted isoindolin-1-one, Solvent-free, Grinding reaction