Studies on synthesis and antiviral activities of 5-substituted pyrimidine acyclic nucleoside phosphonate compounds on HBV

Objective:To study on synthesis and antiviral activities of 5-substituted pyrimidine acyclic nucleoside phosphonate compounds on HBV.Methods: Starting with substituted pyrimidine,we synthesized 8 firstly reported compounds 1a～1h.Preliminary pharmacological test was made on HBV.Results:TThe test results show the inhibitory rate of targeted compounds on HBsAg and HBeAg is normal,but 1d is higher than lamivudine.Conclusion:5-substituted pyrimidine acyclic nucleoside phosphonate compounds keep the normal activities on HBV and introduce long chain of chloroformate at N6 of pyrimidine shows better activity.