A simple, efficient procedure for the one-pot Biginelli condensation reaction of aldehydes, β-ketoesters and urea or thiourea without using any catalyst or solvent is described. Compared to the classical Biginelli reaction conditions, the present method has the advantages of good yields, short reaction times and experimental simplicity. The structure of these compounds was confirmed by analytical M.P. IR, 1HNMR, 13C-NMR, Mass spectral data. The above compounds were evaluated for their antioxidant activity by reducing power and DPPH Free Radical Scavenging Assay. In reducing power the percentage of inhibition of 3, 4-dihydropyrimidin-2(1H)-one derivatives S1, S3, and S4 were found 84.05%,85.50%, 91.30% at 150 μg/mL and for S2 were found to be 94.20% at 125 μg/mL, Similarly in DPPH the percentage of inhibition of of 3, 4-dihydropyrimidin- 2(1H)-one derivatives S1 and S2 were found 77.23% , 82.73% at 125 μg/mL and S3 and S4 were found 84.27%, 63.29% at 150 μg/mL respectively.
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