The Synthesis Of Anti-Hbv Nucleoside Analogues' Drugs

Hepatitis B virus infection is the major reason which cause cirrhosis and hepatocellular carcinoma,and leads to death in the end. It is reported that in the whole world about 350 million people are chrolic carrirers of hepatitis B virus(HBV),each year.acute and chronic HBV infection causes roughtly 1 million deaths.Though safe and effective HBV vaccine can be obtained,the trend of HBV spreading in the world can not decline.Presently ,the drug of treating HBV is interferon in most countries,but low efficiency (30-40%),high treatment expenditure and side effect limit its application .Lamivudine which Glaxo Wellcome company provided in 1999 is the first oral drug for treating HBV ,it can effective suppress HBV-DNA replication ,but after a year course of lamivudine monotherapy,only few patients occur seroconversion to anti-HBV,and easily rebound without drug and resisting drug.So ,new anti-HBV.drug with lowtoxicity imminently required .Adefovir dipivoxiln is a new anti-HBV drug used in clinic.Phase â…  /â…¡ clinical trials demonstrated that it in dose ranging from 5-60mg daily was effective in suppressing HBV replication . PMPA and PMPDAP are adefovir's analogues.Most studies show that they hold stronger suppressing effect than adefovir's.Most of my work is the synthesis of PMPA and PMPDAP,also the design and synthesis of their prodrugs.