Synthesis,Characterization And Bioactivity Test Of 8-Aza-purine Nucleoside Compounds

Purine nucleosides play a paticularly important role in anti-HIV,HBV,tumor.For example: danadoxin,adefovir,entecavir,acyclovir,abacavir have been already used in clinical as purine nucleoside drugs.As we know,Triazole nucleoside is a very good antiviral nucleoside drug.For example,Ribavirin is the most representative triazole nucleoside drug.Ribavirin is the first synthetic triazole nucleoside compound with broad-spectrum antiviral activity and now has been used for anti-hepatitis C virus therapy in clinical.Because of the triazole has an unique five-membered heterocyclic structure and it has been widely used,in pharmaceutical,chemicall,agricultural and other fields,the triazole group arouses great concern of drug researchers.8-azapurine nucleosides have both purine and triazole structures and exhibit better biological activity of antiviral and anticancer in biological systems,thus they have attracted widespread attention from drug researchers.Our laboratory has long been devoted to the development of novel triazole nucleoside compounds in order to find small molecules of nucleoside drugs with antiviral and anti-tumor activity of high efficiency and low toxicity.In this paper,a series of novel 8-azaconucleoside compounds have been designed and synthesized,and the activity of each final compound has been tested.(1)We explored a method to prepare 8-azo xanthine from 2’-β-fluoro-arabin by cascade amidine arylation–intramolecular ester amidation reaction in which palladium as catalyst.We obtained a series of compounds by this method.These compounds were tested for antiviral activity and HCV activity(2)2’-fluoro-2’-methyl-D-arabinofuranosyl-8-azapurine nucleoside compound was synthesized by a series of organic synthesis methods in which 2’-fluoro-2’-methyl-D-arabinofuranose as raw material.Finally,a series of 8-azapurine nucleoside derivatives were obtained by various modifications of the 8-azapurine base.