首页> 外国专利> Process for the preparation of 2,2'-andhydro- and 2'-keto-1-(3',5'-di-o-protected-beta -d-arabinofuranosyl) nucleosides

Process for the preparation of 2,2'-andhydro- and 2'-keto-1-(3',5'-di-o-protected-beta -d-arabinofuranosyl) nucleosides

机译:制备2,2'-和氢-和2'-酮-1-(3',5'-二-o-保护的β-d-阿拉伯呋喃糖基)核苷的方法

摘要

A process for the preparation of compounds of the formula: wherein -Pg and R are protecting groups and B is a nucleobase. The process uses protected nucleobases to form 2,2'-anhydro nucleosides having the formula which are hydrolyzed to 2'-hydroxy intermediates which are then oxidized to the desired 2'-keto compounds. The compounds and intermediates are useful as antiviral and antitumor agents and as intermediates to 2,2'-anhydro-1-(β-D-arabinofuranosyl)cytosine (anhydro-ara-C) and 1-β-D-arabinofuranosylcytosine (Ara-C).
机译:制备下式化合物的方法: <图像文件=“ IMGA0001.GIF” he =“ 23” imgContent =“ chem” imgFormat =“ GIF” wi =“ 45” /> 其中-Pg和R是保护基,B是核碱基。该方法使用受保护的核碱基形成具有下式的2,2'-脱水核苷 <图像文件=“ IMGA0002.GIF” he =“ 23” imgContent =“ chem” imgFormat =“ GIF” wi =“ 45” /> 将其水解为2'-羟基中间体,然后将其氧化为所需的2'-酮化合物。该化合物和中间体可用作抗病毒药和抗肿瘤药,也可用作2,2'-脱水-1-(β-D-阿拉伯呋喃糖基)胞嘧啶(脱水-ara-C)和1-β-D-阿拉伯呋喃糖基胞嘧啶(Ara- C)。

著录项

  • 公开/公告号EP0735045A1

    专利类型

  • 公开/公告日1996-10-02

    原文格式PDF

  • 申请/专利权人 ELI LILLY AND COMPANY;

    申请/专利号EP19960301684

  • 发明设计人 KJELL DOUGLAS PATTON;

    申请日1996-03-12

  • 分类号C07H19/06;

  • 国家 EP

  • 入库时间 2022-08-22 03:46:29

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