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    2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides
    2.
    发明授权
    2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides 失效
    2'-氟呋喃糖苷衍生物及其制备方法2'-氟嘧啶核苷和2'-氟嘌呤核苷

    公开(公告)号：US5817799A

    公开(公告)日：1998-10-06

    申请号：US556713

    申请日：1990-07-23

    申请人： Victor E. Marquez ,  John S. Driscoll ,  Ronald J. Wysocki, Jr. ,  Magbool A. Siddiqui

    发明人： Victor E. Marquez ,  John S. Driscoll ,  Ronald J. Wysocki, Jr. ,  Magbool A. Siddiqui

    IPC分类号： C07H1/00 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61K31/7076 ,  A61P31/12 ,  A61P31/18 ,  C07H13/08 ,  C07H15/04 ,  C07H15/203 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H23/00

    CPC分类号： C07H23/00 ,  C07H19/10 ,  C07H19/16

    摘要： A method of preparing a 2'-fluoro compound of the formula ##STR1## where B is selected from the group consisting of purines and pyrimidines, both of which may be substituted, comprises reacting a compound of the formula II(a) or II(b) ##STR2## where R and R' are as defined in the specification with an acid halide under conditions effective to obtain a halide of the formula ##STR3## where X is a halogen. A silane of the formula B-Si (R").sub.3 where R" is as defined in the specification, is added to this product (III) under conditions effective to obtain a compound of the formula (IV) ##STR4## The compound of formula (IV) is reacted with a reagent selected from the group consisting of ammonia, BCl.sub.3 and ((C.sub.1 -C.sub.10)alkyl).sub.4 NF, under conditions effective to obtain the compound of formula (I). The compounds of formula (I) resulting from these methods exhibit anti-HIV activities and are useful for therapy against the HIV virus.

    摘要翻译： 制备式（I）的2'-氟化合物的方法，其中B选自嘌呤和嘧啶，它们都可以被取代，包括使式II（a）的化合物与式 （IIa）（IIb）其中R和R'如本说明书中所定义，与有效得到式（III）的卤化物的条件下的酰卤相同，其中X 是卤素。 在有效获得式（IV）化合物的条件下，将式B-Si（R“）3的硅烷（其中R”如说明书中所定义）加入到该产物（III）中 IV）在有效获得式（I）化合物的条件下，使式（IV）化合物与选自氨，BCl 3和（（C 1 -C 10）烷基）4 NF的试剂反应。 由这些方法得到的式（I）化合物表现出抗HIV活性，可用于治疗HIV病毒。