Some novel new series of Ethyl-6-((1H-imidazol-1-yl)methyl)-1,2,3,4-tetrahydro-4-aryl-oxopyrimidine-5- carboxylates (6a-f) have been synthesized in two steps. In the first step Ethyl-6-chloromethyl-1,2,3,4-tetrahydro-4- aryl-oxopyrimidine-5-carboxylates (4a-f) ie Biginelli compounds were prepared from Chloroetylacetoacetate, urea and substituted benzaldehyde by using ZrO2 nanopowder under microwave irradiation and the second step, the Biginelli compounds (4a-f) were treated with imidazole (5) in the presence of catalytic amount of NaOH under grinding technique. The present methodology offers several advantages, such as simple procedure with easy workup, short reaction time, high yields and the absence of volatile organic solvents. The structure of the compounds were confirmed by IR, Mass, 1D and 2D NMR like 1H-1H COSY, 1H-13C HSQC spectral analysis and CHN analysis. The synthesized compounds were obeyed the Lipinski’s rule of Five