Studies On The Synthesis Of A Double-target Inhibitor Against Influenza Virus

The synthesis of a dual-targe inhibitor against influenza virus based on zanamivir and ribavirin is studied in this paper.Zanamivir,the first influenza virus neuraminidase(NA) inhibitor,can inhibit both A and B influenza virus.However,the body often produce some other viruses and complications when infected with influenza virus.Therefore, it is difficult to achieve a better therapeutic effect on influenza with more severe symptoms by using zanamivir.Ribavirin is a kind of reverse transcriptase inhibitor with a wide spectrum of antiviral action, and it has a certain inhibitory effect on influenza virus.The inhibitory effect of influenza virus inhibitors on influenza viruses with a single targeting effect is limited.Because ribavirin has broad spectrum, in order to enhance the anti influenza virus activity of zanamivir,In this paper, A broad-spectrum, high efficiency, low toxicity, dual-target anti-influenza virus inhibitor has been synthesized by compounding zanamivir with ribavirin by using linker from Zanamivir Azide Triacetate Methyl Ester,Ribavirin and Hexaethylene Glycolthrough the multi-step organic synthesis reaction.Main content includes the synthesis of zanamivir intermediates(compound 5),the synthesis of polyethylene glycol intermediates(compound 11),The connectionof zanamivir intermediates and polyethylene glycol intermediates, the synthesis of 5'- deoxy- 5'-azide ribavirin and the synthesis of final product(compound 16).Herein, a large amount of(gram degree) the target compound(yield 25%) has been prepared by this method, which can provide adequate material reserves for subsequent biological and pharmaceutical research.