Synthesis and Bioactivity of Dihydropyrimidinone Derivatives Containing Phthalimide Moiety.
Dr. Anandrao A. Kale, Pratiksha Hinge, Pooja Gate
DHPMs, Biginelli Synthesis, Antibacterial analysis, Escherichia coli (E.coli)
A simple and precise synthesis  method that have been used to synthesis of hybrid compounds containing dihydropyrimidinone and phthalimide moieties. The 2-(4-acetyl-phenyl)-1H-isoindole-1,3 (2H)dione.(III) derivatives were synthesized (Scheme-I) by refluxing phthalic anhydride (I) and para-aminoacetophenone (II) in glacial acetic acid for 2 hr. Newly synthesized 2-(4-acetylphenyl)-1H-isoindole-1,3(2H)-dione (III), by refluxing with dimethylformamide-dimethylacetal (DMF-DMA) without solvent for 12 enaminone, 2-{4-[(2E)-3-(dimethylamino)prop-2-enoyl]phenyl}-1H-isoindole-1,3(2H)-dione (IV), The enaminone, 2-{4-[(2E)-3-(dimethylamino)prop-2-enoyl]phenyl}-1H-isoindole-1,3(2H)-dione (IV), used for synthesis of new series of novel Biginelli compounds,5-benzoyl-substituted phenyl-3,4-dihydropyrimidin-2(1H)-one-1H-isoindole-1,3(2H)-dione (Va-Vb), The compounds(V-a to V-d) obtained were identified using physical and spectroscopic 1HNMR, 13CNMR and Mass ) A series of novel dihydropyrimidinone derivatives containing phthalimide moiety were synthesized with good yield, at high purity, and in efficient manner from the enaminone, which was derived from phthalimide by simple and solvent-free method. Compound Va-Vd was tested for antibacterial strain Escherichia coli (E. coli) by Agar well diffusion method. It has been observed that tested compounds Vb and Vc shows good antibacterial activities against Escherichia coli (E.coli) bacterial strains.
Article Details
Unique Paper ID: 151319

Publication Volume & Issue: Volume 7, Issue 12

Page(s): 426 - 431
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