The New No Donor -5 (4h) - Pyridone And Furoxan And Its Nucleoside Derivatives

Furoxans are one important kind of heterocyclic compounds.They are widely used in energetic materials and pharmaceutical fields.However,present studies mainly focus on benzofuroxans and pyrimidofuroxans,research in pyridofuroxans is limited.Considering that pyridine derivatives are good pre-entity in pharmacy and some of them are even integral parts of vitamins or enzyme,this dissertation designed a new compound:4H -[1,2,5]oxadiazolo[3,4-b]pyridine-5-one 1 oxide(4H-pyridofuroxan-5-one in short).With an antibacteria activity which base on the pyridone form,it also has a strengthened combinative ability with endo-acceptor because of the amide form.Besides,furoxan is a good NO-donor.Hereby,this object product would probably has multiple biological activities and has an amazing prospect in pharmaceutical field.If coupled with tetra-acetyl ribose,a non-natural nucleotide is obtained,which has a potential in cure of virus or cancer,This dissertation focused on finding a method to synthesis 4H-pyridofuroxan-5-one. According to the referrence and mechanism analysis,two synthesis methods were designed after taking such factors as cost,inspect methods,reagent characters into consideration: Azidization and nitrogen elimination(the former) and Oxidation by sodium hypochlorite(the latter).During experiments,each synthetic products were characterized by infrared(IR),mass spectra(MS) and ~1H nuclear magnetic resonance(NMR).Each step was analysed in mechanisms.It proved that both synthesis methods were feasible.The former one was comparatively better than the latter one,with a higher general yield and more convenient operations,the latter method still need modification.Furthermore,biological activity tests showed that the object product and its nucleotide derivative had an anti-tumour activity.