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Hepatitis B virus infection, is caused by cirrhosis of the liver and liver cancer , the last one of the main factors leading to death . It is reported that the world now has 350 million hepatitis B virus carriers , each year one to two million hepatitis B patients due to disease progression and death. Although currently available hepatitis B vaccine safe and effective , but the world trend of the spread of hepatitis B and did not decline. Currently, most countries around the world for the treatment of hepatitis B drugs for anti-interferon , but its low efficiency ( 30-40% ) and high cost of treatment and side effects limit its application . 1999 Glaxo Wellcome company listed lamivudine treatment of hepatitis B is the first oral medication , although it can effectively inhibit HBV-DNA replication, but year after treatment , only a minority of the patients Hbe antigen seroconversion , and there easy rebound after stopping and drug issues. Therefore, an urgent need to find new effective antiviral drugs. Adefovir dipivoxil (Adefovir Dipivoxil) was approved by the FDA in 2002 for the treatment of chronic hepatitis B. Clinical studies show that it has a good anti -virus effect, and that there was no resistance, which indicates that it has good application prospects. PMPA is adefovir Indica PMPDAP analogues , their synthesis and preparation of PMPA prodrugs in foreign countries in recent years has begun. Studies have shown that they have good inhibitory effect of HBV and比阿德福韦stronger cytotoxic . There is no domestic PMPA, PMPDAP prodrug synthesis and study them . In particular the preparation of prodrug PMPDAP , after a comprehensive literature search , the current worldwide PMPDAP prodrug is not reported. The main work of this paper are: ( 1 ) synthesis PMPA, PMPDAP, and to improve its part of the process ; ( 2 ) to PMPA, PMPDAP prodrug for the original drug synthesis . After nearly two years of experiments : ( 1 ) opened the PMPA, PMPDAP synthetic route ( a total of 12 steps ) , and improved its part of the process : ( 2 ) synthesis of 7 prodrug ( of which 6 are new compounds ): PMEA prodrug 1 : PMPA prodrugs 3 ; PMPDAP prodrug 3 . Currently being patented. Due to the need also synthesized adefovir dipivoxil (Adefovir Dipivoxil).
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