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The Pharmaceutical Society of Korea (대한약학회)
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Synthesis and Antiviral Activity of Novel Exomethylene Cyclopropyl Pyrimidine Nucleosides

  • Kook, Min-Chul (Department of Medicinal Chemistry, College of Pharmacy, Chonnam National University) ;
  • Kim, Gu (Department of Medicinal Chemistry, College of Pharmacy, Chonnam National University) ;
  • Kwak, Eun-Yee (Department of Medicinal Chemistry, College of Pharmacy, Chonnam National University) ;
  • Hong, Joon-Hee (Department of Medicinal Chemistry, College of Pharmacy, Chosun University) ;
  • Lee, Chong-Kyo (Pharmaceutical Screening Center, Korea Research Institute of Chemical Technology) ;
  • Choi, Bo-Gil (Department of Medicinal Chemistry, College of Pharmacy, Chonnam National University)
  • Published : 2002.12.01
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Abstract

A series of novel exomethylene cyclopropyl nucleosides have been synthesized starting from Feist's acid. Classical nucleophilic substitution conditions ($K_2CO_3$, 18-crown-6) of the tosylate 2 as well as Mitsunobu reaction (DEAD, $PPh_3$) of alcohol 1 with pyrimidine bases afforded a series of novel cyclopropyl nucleosides. Compound 4b displayed moderate anti-HBV activity without any cytotoxicity up to $100{\;}{\mu}M$.

Keywords

References

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