One pot, two-step synthesis of pyrimidine derivatives via arylamins, benzonitriles, benzaldehydes and Meldrum s acid

Pyrimidines and their derivatives, a type of important N-containing heteroaromatic compounds, were found in a large number of pharmacologically active compoundsand natural products such as alkaloids and pharmaceutical drugs, anticancer, antiinflammatory, antimalarial, antiviral agents [1], [2]. Herein, we describe efficient method to the synthesis of pyrimidine derivatives via appropriate arylamine 1 and benzonitrile 2 and the mixture was stirred at 120 oC for 1h under solvent-free conditions. Then a mixture of appropriate benzaldehyde derivatives 3 and meldrum s acid 4 was stirred in acetonitrile at reflux conditions for 24 h. After completion of the reaction, determined by TLC, the solvent was removed under reduced pressure, and the viscous residue was purified by thin-layer chromatography using n-hexane– ethylacetaat as eluent to give 5 products (Fig 1). All the synthesized compounds were known by 1H and 13C NMR, IR and melting points.