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CN105175469A 6-叔丁基-8-二苯基磷氧基-2′-氟阿糖嘌呤核苷及其制备方法和应用 无效 - 撤回

  • 专利标题： 6-叔丁基-8-二苯基磷氧基-2′-氟阿糖嘌呤核苷及其制备方法和应用
  • 专利标题（英）： 6-tert-butyl-8-diphenylphosphinyloxy-2'-F-ara-purine nucleoside as well as preparation method and application thereof
  • 申请号： CN201510646020.0
    申请日： 2015-10-09
  • 公开(公告)号： CN105175469A
    公开(公告)日： 2015-12-23
  • 发明人: 孙莉萍 , 夏然 , 张家洋
  • 申请人： 新乡学院
  • 申请人地址： 河南省新乡市金穗大道191号
  • 专利权人： 新乡学院
  • 当前专利权人： 新乡学院
  • 当前专利权人地址： 河南省新乡市金穗大道191号
  • 代理机构： 北京汉昊知识产权代理事务所
  • 代理商 冯谱
  • 主分类号： C07H19/19
  • IPC分类号： C07H19/19 ;  C07H1/00 ;  A61K31/708 ;  A61P35/02
6-叔丁基-8-二苯基磷氧基-2′-氟阿糖嘌呤核苷及其制备方法和应用
摘要：
本发明提供了6-叔丁基-8-二苯基磷氧基-2′-氟阿糖嘌呤核苷的制备方法及应用。发明人在大量的化合物合成和活性筛选中发现，6-叔丁基-8-二苯基磷氧基-2′-氟阿糖嘌呤核苷具有很好的抗HL-60细胞活性。这种化合物的结构式如式I：同时，我们对其合成方法也进行了研究。解决了现有的合成方法存在着步骤多、收率低、操作繁琐等缺点，如：(1)金属催化偶联反应；(2)6-氢嘌呤核苷的自由基反应。这两类方法均使用到过渡金属催化剂(如钯、镍、钌等)或者难以获得的原料(如格利雅试剂、有机锌试剂等)。同时提供一种高效的6-叔丁基-8-二苯基磷氧基-2′-氟阿糖嘌呤核苷的方法。
摘要（英）：

The invention provides 6-tert-butyl-8-diphenylphosphinyloxy-2'-F-ara-purine nucleoside as well as a preparation method and an application thereof. Synthesis and activity screening of a large number of compounds prove that 6-tert-butyl-8-diphenylphosphinyloxy-2'-F-ara-purine nucleoside has good activity resistant to HL-60 cells. The structural formula of the compound is shown as a formula I, and meanwhile, synthetic methods of the compound are also researched. The defects of multiple steps, low yield, complex operation and the like of conventional synthetic methods, such as (1) metal-catalyzed coupling reaction and (2) free radical reaction of 6-hydrogen purine nucleoside, are overcome. Both methods utilize transition metal catalysts such as palladium, nickel, ruthenium and the like or raw materials such as a Grignard reagent, an organic zinc reagent and the like which are difficult to acquire. Meanwhile, the efficient preparation method of 6-tert-butyl-8-diphenylphosphinyloxy-2'-F-ara-purine nucleoside is provided.

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