Matrine Derivatives With The Sulfur Ethers Compounds Synthesis

The purpose of the structure of modification and restructuring of the natural medicine research that include the following points:improve the selectivity of drug, improve the pharmacological activities of drug, increase the stability of drug, prolong the drug duration, improve the solubility of drug and lower the poison of drug. We know about the structure of some public drugs that have similarities portion. For example, the different groups are linked through the carbon and heteroatom bond and it include heterocyclic structure. So we introduce the heterocyclic moiety with pharmacological activities by the Michael addition reaction in13-position. The novelty structural modification is that formed a new chiral center in13-position and introduced heterocyclic moiety by the carbon sulphur bond. We expect to have a good application in pharmacological fied.Sulfhydryl compounds are important industrial raw material and important drug intermediates. The synthesis technologies are also becoming the focus of attention all over the world. The disulfides that derived from sulfhydryl compounds become the research focus in recent years. Disulfides are important compounds from both synthetic and biological viewpoints. First the sulfhydryl compound was prepared. Then a series of disulfides were obtained which were oxidized with sodium periodate and hydrogen peroxide. At last we made the further work to synthetize the asymmetry disulfides.This thesis is comprised of three parts as follows:In the chapter one:we summarized the study progress of the nature medicine firstly, emphasizing to introduce the biological characters and pharmacological activities of the alkaloids. The application and synthesis methods were introduced in the research of sulfhydryl compounds. The synthesis methods and function of the disulfides were also introduced.In the chapter two:The13-position of sophocarpine was introduced five kinds of sulphur compounds by the Michael addition reaction. The five kinds of matrine derivatives were successfully obtained. We designed an experiment to synthesize two novel derivatives of matrine. The method was confirmed to be novel for one-pot preparation of matrine dithiocarbamate. In the chapter three:The a-thiol-4-ethylbenzoic acid with4-ethylbenzoic acid was successfully synthesized. Then the2-mercaptopyridine,2-aminothiophenol,2-mercaptobenzimidazole,2-mercaptobenzoxazole and5-mercapto-1-methyltetrazole with sodium periodate and hydrogen peroxide were respectively oxidized.The five symmetrical disulphides were easily obtained. We made the further work to study the asymmetric disulphides by using three kinds of methods.