Abstract: A specific efficient method of synthesis of biologically active analogues of the title compound from acetylene dicarboxylate, aniline and various aromatic aldehydes catalyzed by citric acid by one-pot mortar-pestle grinding is described. The short time synthesis is characterized by high yields and comparable with the similar mechano-chemical process of planetary ball-milling. Easy isolation of the products without involving separation methods makes this green synthesis to be cost-efficient. © 2021, Pleiades Publishing, Ltd.