Synthesis Of Some 1,2,4-triazole Derivatives And The Research Of New Catalyst For Biginelli Reaction

Cancer is one of the most deadly diseases in the world. There are a lot of people die from the diseases related to cancer every year, and the mortality rate is second only to cardiovascular and cerebrovascular diseases. The rate still keeps on rising. At present, the antitumor effect of chemical drugs has been proven exactly. However, because of the cytotoxicity, this kind of drugs can induce great toxic and side-effect and bring the drug resistance by long term using. Therefore, their use of the clinical application is confined. So people urgently need to find the novel potent, high selective, and less toxic anticancer agents.It is reported that a lot of triazole derivatives are associated with many types of biological properties. So according to the bioresearch about the 1,2,4-triazole-5-thiones derivatives and the research of synthesis and activity test about 1,3,4-oxadiazole-2-thiones derivatives and 1,2,4-triazole-5-thiones derivatives our topic did before, more types of derivatives were synthesized, including benzoyl amino acid oxadiazoles, benzoly amino acid triazoles and L-tartaric acid triazoles. The structures of the 11 novel compounds were confirmed by IR, MS and NMR.In recent years, the research shows that some dihydropyrimidin ketones have important pharmacological activities, and these compounds were often synthesized by the classical Biginelli condensation reaction. The product of this reaction,3,4-dihydropyrimidin-2(1H)-ones(DHPMs), were prepared by condensation using acetyl ethyl acetate, aromatic aldehydes and urea with concentrated hydrochloric acid catalyzed. But this synthetic method involves a long reaction time, harsh reaction conditions or low yields. So people improve the reaction conditions, such as changing the suitable catalyst and using other synthetic method. Some high yield synthetic routes were found. In this essay, according to the study of Biginelli reaction mechanism, a new catalyst, L-camphor sulfonic acid, were found. This catalyst can make the reaction have a high yield, and the product can be separated and purified easily. With changing the solvent, the optical activity of the reaction product which had been purified was determined. And then the relationship between the reaction conditions and the optical activity of the product was discussed.