Green Expedient Synthesis of Pyrimidine Derivatives via Chalcones and Evaluation of their Anthelmintic Activity

Abstract

Abstract: Objective: In the present study, we focused on the environment-friendly processes used for the preparation of pyrimidine derivatives with pharmacological properties. In this regard, microwave heating is used as the alternative energy sources to synthesize a series of pyrimidine derivatives by the condensation of chalcones with urea under basic conditions. Chalcones were synthesized by Claisen-Schimidt condensation of acetophenone with various substituted benzaldehyde in the presence of ethanolic potassium hydroxide solution. Methods: The IR, 1H-NMR, mass spectra and CHN analyses confirmed the structure of the prepared compounds. Shorter reaction time, environment friendly procedure and excellent yields are the advantages of microwave synthesis. The newly synthesized pyrimidine derivatives were screened for their anthelmintic activity and found to have moderate to considerable activity as compared to the standard drug. Results: Some of the synthesized compounds exhibited significant anthelmintic activity. Compound 4e with electron withdrawing groups was found to be highly potent among the series. This attempt will lead to an increased number of new and sustainable methods for the synthesis of biologically-active pyrimdine derivatives. Keywords: Anthelmintic activity, Chalcone, Claisen-schmidt reaction, Green synthesis, Pyrimidine.