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).
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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” /> Chemistry> 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” /> Chemistry> 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)。
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