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

Akbaş E., Berber I., AKYAZI I., ANIL B., YILDIZ E.

LETTERS IN ORGANIC CHEMISTRY, vol.8, no.9, pp.663-667, 2011 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 8 Issue: 9
  • Publication Date: 2011
  • Doi Number: 10.2174/157017811799304287
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.663-667
  • Keywords: Antimicrobial substances, microwave-assisted, multicomponent reactions, DERIVATIVES
  • Van Yüzüncü Yıl University Affiliated: Yes


Various pyrimidine derivatives (1a-c) were synthesized using the Biginelli three component cyclocondensation reactions of a beta-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.