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Alpha-1-phosphorylated-2-deoxy-2-fluoroarabinoside and process for producing 2'-deoxy-2'-fluoro-beta-d-arabinonucleoside
Alpha-1-phosphorylated-2-deoxy-2-fluoroarabinoside and process for producing 2'-deoxy-2'-fluoro-beta-d-arabinonucleoside
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机译:α-1-磷酸化的2-脱氧-2-氟阿拉伯糖苷和生产2'-脱氧-2'-氟β-d-阿拉伯糖苷的方法
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摘要
A method for producing 2′-deoxy-2′-fluoro-β-D-arabinonucleoside represented by formula (II): [F3] (wherein B represents a base), in particular, 2′-deoxy-2′-fluoro-β-D-arabinopurinenucleoside, which method comprises causing a nucleoside phosphorylase to act on α-1-phosphorylated-2-deoxy-2-fluoroarabinoside represented by formula (I): [F1] or a mixture of α- and β-isomers of 1-phosphorylated-2-deoxy-2-fluoroarabinoside represented by formula (V′): [F2] and on a base. The compound can be produced at high yield and in a convenient and highly stereoselective manner.
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机译:式(II)所示的2'-脱氧-2'-氟-β-D-阿拉伯糖核苷的制造方法:[F3] <图像alt =“嵌入式图像” file =“ US20070135627A1-20070614-C00001.GIF” he =“ 20.24mm” id =“ EMI-C00001” imgContent =“ chem” imgFormat =“ GIF” wi =“ 49.45mm” /> Chemistry>(其中B代表碱基),特别是2'-脱氧-2'-氟-β-D-阿拉伯嘌呤核苷,该方法包括使核苷磷酸化酶作用于α-1-磷酸化-2-脱氧-2-氟阿拉伯糖苷由式(I)表示:[F1] <图像alt =“嵌入式图像” file =“ US20070135627A1-20070614-C00002.GIF” he =“ 20.24mm” id =“ EMI-C00002” imgContent =“ chem” imgFormat =“ GIF” wi =“ 54.78mm” /> Chemistry>或由式(V')表示的1-磷酸化的2-脱氧-2-氟阿拉伯糖苷的α-和β-异构体的混合物:[F2] <图像alt =“嵌入式图像” file =“ US20070135627A1-20070614-C00003.GIF” he =“ 20.32mm” id =“ EMI-C00003” imgContent =“ chem” imgFormat =“ GIF” wi =“ 55.63mm” /> Chemistry>并在一个基础上。该化合物可以高产率且以方便且高度立体选择性的方式生产。
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