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    1-Alpha-Halo-2,2-Difluoro-2-Deoxy-D-Ribofuranose Derivatives and Process for the Preparation Thereof
    12.
    发明申请
    1-Alpha-Halo-2,2-Difluoro-2-Deoxy-D-Ribofuranose Derivatives and Process for the Preparation Thereof 失效
    1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物及其制备方法

    公开(公告)号：US20070238865A1

    公开(公告)日：2007-10-11

    申请号：US11572790

    申请日：2005-06-21

    申请人： Jaeheon Lee ,  Gha Park ,  Moonsub Lee ,  Han Kim ,  Hyo-Jeong Bang ,  Young-Kil Chang ,  Gwan Lee

    发明人： Jaeheon Lee ,  Gha Park ,  Moonsub Lee ,  Han Kim ,  Hyo-Jeong Bang ,  Young-Kil Chang ,  Gwan Lee

    IPC分类号： C07H15/00

    CPC分类号： C07H3/08

    摘要： 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.

    摘要翻译： 具有用联苯基羰基保护的3-羟基的式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物是可以通过简单的方法容易地纯化的固体，例如 重结晶，因此可以有利地用作大量制备吉西他滨的中间体。 此外，式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物可以使用式（V）化合物作为中间体以高立体选择性制备。