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Synthesis of telbivudine 3'-O-acetyl-5'-O-phenyl-N-alkylphosphramidates and evaluation of their anti-HBV activities

Liang-Liang Shi, Hai-Nan Wei, Chang-Mei Cheng*, Lang-Qiu Chen*, Yi-Gang Tong   

  1. 1. College of Chemistry, Key Laboratory of Environmental Friendly Chemistry and Application, the Ministry of Education, Xiangtan University, Xiangtan 411105, China
    2. Key Laboratory of Bioorganic Phosphorus and Chemical Biology, the Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, China
    3. State Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, China

  • Received:2011-03-25 Revised:2011-05-30 Online:2011-09-20 Published:2011-09-20
  • Contact: Chang-Mei Cheng*, Lang-Qiu Chen*

Abstract: A series of telbivudine 3'-O-acetyl-5'-O-phenyl-N-alkylphosphramidate derivatives have been synthesized and their structures were confirmed by EI-MS, 1H NMR and 13C NMR. We evaluated their anti-HBV activity in vitro. Two compounds 6d and 6f, turned out to be more active than telbivudine.

Key words: Telbivudine, Phosphramidates, Synthesis

CLC Number: 

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