• Title/Summary/Keyword: Feist′s acid

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Synthesis and Antiviral Activity of Novel Exomethylene Cyclopropyl Pyrimidine Nucleosides

  • Kook, Min-Chul;Kim, Gu;Kwak, Eun-Yee;Hong, Joon-Hee;Lee, Chong-Kyo;Choi, Bo-Gil
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.790-794
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    • 2002
  • 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 $100{\;}{\mu}M$.