Synthesis And Character Study On Phosphorus Disubstituted Piperizine Deritives

Piperazine derivatives have attracted many attentions for their broad spectrum of biological activities such as anti-bacterial, anti-hypertension, anti-cancer, anti-pain, anti-depressant etc. Therefore the research and development of drugs containing piperazine derivatives has become very active. And some drugs have been utilized therapeutically. The study shows that the biological activities of piperazine derivatives are highly depended on the substitutes in 1,4-position of piperazine rings. According to the pharmacological principle of stacking, such biologically active groups as N-phosphoryl amino acid, thiosemicarbazone and aroyl are introduced to piperazine rings, with a view to get drugs with better biological activity.In this dissertation, two synthesis routes were adopted. Within five and six steps accordingly ten target molecules with aroyl and N-phosphoryl amino acid substitutes and nine target molecules with thiosemicarbazone and N-phosphoryl amino acid substitutes were synthesized respectively. All these nineteen compounds have not been reported in literature, and four intermidates are new compouds too.The structures of nineteen compounds were confirmed by 1H NMR,13C NMR,31P NMR,IR and MS. Weak interactions between target molecules and insulin,cytochrome and lysozyme were studied and found that the interactions between these compounds and lysozyme is distinguished. The synthesis routes are shown as following schemes.