Catalyst-Free Synthesis of 3-(2-Quinolinemethylene)-Substituted Isoindolinones in Water

Article abstract of DOI:10.1055/s-0037-1609491

A facile and environmentally benign approach toward the synthesis of novel 3-alkyl-substituted isoindolinones by three-component reactions of 2-formylbenzoic acids, primary amines and 2-methylazaarenes in water under catalyst- and additive-free conditions is described. This protocol features the direct construction of multiple C-N and C-C bonds via a tandem Mannich-type reaction and intramolecular cyclization in a one-pot fashion, affording the desired 3-(2-quinolinemethylene)-substituted isoindolinones in high to excellent yields.