Microwave-Assisted Synthesis of Tetrahydropyrimidines via Multicomponent Reactions and Evaluation of Biological Activities

Title: Microwave-Assisted Synthesis of Tetrahydropyrimidines via Multicomponent Reactions and Evaluation of Biological Activities

Volume: 8 Issue: 9

Author(s): Esvet Akbas, Ismet Berber, Inci Akyazi, Baris Anil and Ela Yildiz

Affiliation:

Keywords: Antimicrobial substances, microwave-assisted, multicomponent reactions, acetoacetate, Biginelli reactions, ethanol, dihydropyrimidine, arylaldehyde, benzaldehyde, antiinflammatory

Abstract: Various pyrimidine derivatives (1a-c) were synthesized using the Biginelli three component cyclocondensation reactions of a β-diketone, arylaldehyde, and thiourea, under microwave irradiation and conventional conditions. The acetylation of compound 1a gave 3-acetyl thioxopyrimidin 2. Also, thiazolopyrimidine (3) and (4) derivatives were obtained by a simple one-pot condensation reaction of starting compounds 1a, and 1b with 2-bromopropionic acid. The prepared compounds were screened for their antimicrobial activities against Gram-positive, Gram-negative bacteria and fungi using micro dilution procedure. The results of the study showed that the compound 4 was effective and selective for antimicrobial activity against the tested bacteria and fungi. Thus, we suggested that the compound 4 might be a new potential antimicrobial substance for bacteria and fungi.

Cite this article as:

Akbas Esvet, Berber Ismet, Akyazi Inci, Anil Baris and Yildiz Ela, Microwave-Assisted Synthesis of Tetrahydropyrimidines via Multicomponent Reactions and Evaluation of Biological Activities, Letters in Organic Chemistry 2011; 8 (9) . https://dx.doi.org/10.2174/157017811799304287