Intermediate and process for preparing of β- anomer enriched 21-deoxy,21,21-difluoro-D-ribofuranosyl nucleosides
    3.
    发明授权
    Intermediate and process for preparing of β- anomer enriched 21-deoxy,21,21-difluoro-D-ribofuranosyl nucleosides 有权
    制备富含β-异头物的21-脱氧,21,21-二氟-D-呋喃核糖核苷的中间体和方法

    公开(公告)号:US07235647B2

    公开(公告)日:2007-06-26

    申请号:US11332830

    申请日:2006-01-13

    CPC classification number: C07H19/073 C07H13/08

    Abstract: The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the β-enriched anomer of gemcitabine hydrochloride of formula (IIb) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).

    Abstract translation: 本发明提供高度立体选择性,简单和经济的糖基化方法,其用于制备富含β-端基异构体的2-DIO-2 1,1/2 SUP 式(II)的-D-呋喃核糖二基二氟核苷及其生理学上可接受的盐,特别是纯度> 99%的式(IIb)的吉西他滨盐酸盐的β-富集的端基异构体通过使用式(II)的新型三氯乙酰亚氨酸酯 (一世)。

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