An efficient and simple three-component domino synthesis of some new dihydropyrimidines (DHPMs) from aromatic aldehydes, 1,3-dicarbonyl compounds and N-(3-chloro-4-fluorophenyl)urea using molecular iodine as catalyst is described. The 1-substituted dihydropyrimidines were isolated in good to excellent yields (78-90%) within a short reaction time (4-6 h) at ambient temperature. The biological evaluation revealed that the newly synthesized compounds (4a-i and 5a-i) exhibited moderate antimycobacterial activity against Mycobacterium tuberculosis H(37) RV.

Ring closure reactions O 0130Synthesis and Antimicrobial Activity of Some New Cyanopyridine and Cyanopyrans Towards Mycobacterium tuberculosis and Other Microorganisms. -A series of 9 compounds of each type (III), (V), and (VI) is prepared. Some of them show moderate antitubercular or antimicrobial activities. -(VYAS, D. H.; TALA, S. D.; AKBARI, J. D.; DHADUK, M. F.; JOSHI, K. A.; JOSHI*, H. S.; Indian J. Chem., Sect. B: Org. Chem. Incl. Med. Chem. 48 (2009) 6, 833-839; Dep. Chem., Saurashtra Univ., Rajkot 360 005, India; Eng.) -M. Bohle 42-024

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A simple, efficient and modified Biginelli procedure was carried out for the synthesis of tetrahydropyrimidines 4a-o by a solvent-free and catalyst-free condition, by the condensation of 1,3-dicarbonyl compound 1, arylaldehydes 2 and urea/thiourea 3. Neat reactants subjected to microwave irradiation gave the required products more quickly and in better yield in comparison to traditional methodologies. The observed yields and improvement in reaction rates are due to the solvent free conditions coupled with the use of microwave radiation.