Design, Synthesis Of 2-thioxo-hexahydroquinazolin-5-one Derivatives By Biginelli Reaction

Objective: 3,4-dihydropyrimidin-2-thione is benzodihydropyrimidine thione compounds, which has wide range of biological activities in prevention of anti-cardiovascular disease, antimicrobial, anti-inflammatory and anti-tumor. So, a series of benzodihydropyrimidine thione derivatives, which are oxygen and sulfur heterocyclic compounds, were design and synthesis.Method:3,4-dihydropyrimidin-2-thione derivatives were synthesized via Biginell reaction catalyzed by acid, with Thiourea, urea, cyclohexanedione, and aromatic aldehydes as reactant. And the reation conditions were discussed and optimized.Result:1,3,4-dihydropyrimidin-2-thione derivatives were synthesized, with thiourea as reaction, and used nuclear magnetic spectroscopy (1H-NMR and 13C-NMR) and mass spectrometry to confirm the products structure.2,discuss catalyst to control the selection and quantity, reaction time and ratio of reactants3,9-phenyl-hexahydroxanthene-1,8-dione derivatives were synthesized, with urea as reactant, and used nuclear magnetic spectroscopy (1H-NMR and 13C-NMR) and mass spectrometry to confirm the products structure.Conclusions: A series of benzodihydropyrimidine thione derivatives, which are oxygen and sulfur heterocyclic compounds, were designed and synthesized. Additionally, 9-phenyl-hexahydrogen hybrid anthracene-1,8-dione derivatives were unexpectedly synthesized.