Eco-friendly one-pot, three-component synthesis of novel derivatives of kojic acid by the Mannich-type reaction under solvent-free ball-milling conditions

摘要

A novel series of aminokojic acid derivatives were efficiently synthesized by one-pot condensation of kojic acid, aromatic aldehydes and heteroaromatic amines in the presence of cerium(III) sulphate as an efficient and recyclable catalyst in ball-milling under solvent-free conditions at room temperature. This synthesis method offers several advantages, including a green and eco-friendly protocol, operational simplicity, mild reaction conditions, short reaction time, higher yields and easy workup procedures. The workup of these very clean reactions involves only a simple washing with acetone/cold water. The catalytic system can be reused several times with no loss of activity.