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An efficient and facile synthesis of substituted pyrimidine derivatives through Biginelli type reaction was achieved in high yields via one-pot reaction of aromatic aldehydes, active methylene compounds and urea or thiourea in the presence of choline chloride- urea mixture as a deep eutectic solvent or cerium (IV) ammonium nitrate (CAN) as a catalyst at different conditions. The reaction was carried out using different ratio of CAN in different solvents to determine the optimum conditions. In addition, 2-mercapto-6-oxo- 4-(thiophen-2-yl)-1,6-dihydropyrimidine-5-carbonitrile was employed in the synthesis of pyrimidinylhydrazide and its corresponding hydrazone. The structural formula of all derivatives was confirmed and characterized by their elemental analyses and spectral data (IR, MS, 1H NMR, 13C NMR).

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An efficient and facile green synthesis of chalcone derivatives 1a-d was achieved by treatment of aromatic aldehydes with 2-acetylthiophene in the presence of choline chloride-urea mixture as a deep eutectic solvent. Chalcone 1a was used as a reactive key precursor to design a series of bio-active heterocycles such as pyrimidine, pyrazoline, pyridine, pyridopyrimidine and naphthyridine. The Structural formula of derivatives were confirmed and characterized by their elemental analyses and spectral data (IR, MS, 1 H NMR, 13 C NMR). In addition, the synthesized derivatives were evaluated for their antimicrobial activities, it was found that compounds 3, 8 and 9a exhibited potent antifungal activity in comparison with the standard drug. Cytotoxicity against breast cancer (MCF7) was screened also and most compounds showed low to moderate activity. The results of the viral screening against HBV of selected compounds indicated that compounds (9b, 15), 8, (3, 6), and 5 showed moderate viral replication inhibition.

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