The Synthesis Of New 2-Thio-4-Pyrimidinones

Heterocycles containing nitrogen and sulfur elements have lots of applications in wide areas including pesticide, pharmaceutical and so on. They have attracted people's attention. Consequently, exporing a novel way to synthesize new heterocycles has a good value of research. The thesis has studied the synthesis of new 2-thio-4-pyrimidinones.The thesis consists of three chapters.In chapter one, we mainly made a review of the progress about the synthesis and applications of 2-thio-4-pyrimidinones in recent years.In chapter two, cyclopentanone, cyclohexanone were used to synthesize novel acylthiourea derivatives containing cyclopentene ring and cyclohexene ring with a series reations, which is a pre-prepared unit to synthesize 4-pyrimidinone. The structure was confirmed through X-ray diffraction. The preliminary bioassay test indicated that some compunds exhibited a certain antitumor activity to A549 cells in vitro by MTT assay. Compound 10h exhibited most effective against A549 cells with IC50 values of 0.03 mmol/L. The study on the bioassay laid the foundation for the further biologically research of the new compounds.In chapter three, we reported the synthesis of 2-thio-4-pyrimidinones in (CH3)3COK/DMSO. The method we explored had the followings:shorter reaction time, higher yields, good selectivity and less by-products. The compounds we reported are new compounds and we comfirmed the structure through X-ray diffraction.