高等学校化学学报

高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (S1): 68.

• Organic Synthesis Chemistry • 上一篇    下一篇

Synthesis of 2-ethyl-3-Hydroxy-4-Pyridone Nucleosides

Chen Weimin1, Zeng Longmei2   

  1. 1. Institute of Pharmaceutical Sciences, The First Military Medical University, Guangzhou 510515;
    2. Department of Chemistry, Zhongshan University, Guangzhou 510275
  • 出版日期:1998-12-31 发布日期:1998-12-31
  • 基金资助:
    This research was supported by the natural sciences foundation of Guangdong province

Synthesis of 2-ethyl-3-Hydroxy-4-Pyridone Nucleosides

Chen Weimin1, Zeng Longmei2   

  1. 1. Institute of Pharmaceutical Sciences, The First Military Medical University, Guangzhou 510515;
    2. Department of Chemistry, Zhongshan University, Guangzhou 510275
  • Online:1998-12-31 Published:1998-12-31
  • Supported by:
    This research was supported by the natural sciences foundation of Guangdong province

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摘要： The hydroxypyridones were found to have wide biological activities such as they can be used as iron chelators for the treatment of iron overload of transfusion-dependant patients[1]. Some hydroxypyridones were discovered to possess moderate reproducible activity against murine P-388 leukemia[2] and showed antimalarial activity[3]. Besides some nucleoside of hydroxypyridones exhibit antitumor activity[4]. The 2-ethyl-3-hydroxy-4-pyridone nucleosides were synthesized by direct condensation of the silylated 2-ethyl-3-hydroxy-4-pyridone with 1,2,3,5-tetra-o-acetyl-β-D-ribofuranose using trimethylsilyl triflate(Me3SiOTf) as catalyst. Deblocking of the protected ribofuranosyl nucleosides was performed by the standard methods.

Abstract: The hydroxypyridones were found to have wide biological activities such as they can be used as iron chelators for the treatment of iron overload of transfusion-dependant patients[1]. Some hydroxypyridones were discovered to possess moderate reproducible activity against murine P-388 leukemia[2] and showed antimalarial activity[3]. Besides some nucleoside of hydroxypyridones exhibit antitumor activity[4]. The 2-ethyl-3-hydroxy-4-pyridone nucleosides were synthesized by direct condensation of the silylated 2-ethyl-3-hydroxy-4-pyridone with 1,2,3,5-tetra-o-acetyl-β-D-ribofuranose using trimethylsilyl triflate(Me3SiOTf) as catalyst. Deblocking of the protected ribofuranosyl nucleosides was performed by the standard methods.

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