化学学报 ›› 2009, Vol. 67 ›› Issue (15): 1822-1824. 上一篇    

研究简报

3’-叠氮-3’-脱氧胸苷-α-羟基膦酸酯衍生物的合成

任玉杰*,a 孙笑宾*,a 舒春风a 奚才明a 肖 强b
刘 马a 赵玉芬c

  

  1. (a华东理工大学化学与分子工程学院 上海 200237)
    (b江西科技师范学院有机功能分子研究所 南昌 330013)
    (c清华大学生命有机磷化学和化学生物学教育部重点实验室 北京 100084)

  • 收稿日期:2008-10-10 修回日期:2009-02-16 出版日期:2009-08-14 发布日期:2009-08-14
  • 通讯作者: 孙笑宾

Synthesis of 3’-Azido-3’-Deoxythymidine-α-Hydroxyphosphonate Derivatives

Ren, Yujie*,a Sun, Xiaobin*,a Shu, Chunfenga Xi, Caiminga Xiao, Qiangb
Liu, Maa Zhao, Yufenc
  

  1. (a Department of Chemistry, East China University of Science and Technology, Shanghai 200237)
    (b Institute of Organic & Functional Molecules, Jiangxi Normal College of Science and Technology, Nanchang 330013)
    (c Education Ministry Key Laboratory of Bioorganic Phosphorus and Chemical Biology, Tsinghua University, Beijing 100084)
  • Received:2008-10-10 Revised:2009-02-16 Online:2009-08-14 Published:2009-08-14
  • Contact: Sun, Xiaobin

在碱性条件下, 抗病毒核苷衍生物3’-叠氮-3’-脱氧胸苷(AZT)-5’-氢亚膦酸二酯与芳香醛加成反应得到4个3’-叠氮-3’-脱氧胸苷-α-羟基膦酸酯类衍生物, 通过31P NMR, 1H NMR, ESI-MS及元素分析对其结构进行了表征确认.

关键词: 3’-叠氮-3’-脱氧胸苷, 氢亚膦酸二酯, α-羟基膦酸酯, 抗病毒

Four 3’-azido-3’-deoxythymidine (AZT)-α-hydroxyphosphonate derivatives were prepared by the addition of diverse aryl aldehyde to the corresponding AZT-5’-yl H-phosphonate diester in the presence of base catalyst. The structures of all products were confirmed by 31P NMR, 1H NMR, ESI-MS and elemental analyses.

Key words: AZT, H-phosphonate diester, α-hydroxyphosphonate, anti-virus