知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

25 条记录 (耗时 0.023 秒)

    2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides
    6.
    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。

    Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors
    10.
    发明授权
    Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors 失效
    导致氟化逆转录酶抑制剂制备的关键中间体的非对映选择性过程

    公开(公告)号：US5498719A

    公开(公告)日：1996-03-12

    申请号：US189095

    申请日：1994-01-31

    申请人： Victor E. Marquez ,  John S. Driscoll ,  Magbool A. Siddiqui

    发明人： Victor E. Marquez ,  John S. Driscoll ,  Magbool A. Siddiqui

    IPC分类号： C07D317/26 ,  C07D317/30 ,  C07D413/06

    CPC分类号： C07D413/06 ,  C07D317/26 ,  C07D317/30

    摘要： The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-.alpha.-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.

    摘要翻译： 本发明提供了一种关键前体的新型合成途径，即用于制备FddA的（S，S）-α-氟-2,2-二甲基-1,3-二氧戊环-4-丙酸酯 FddC。 即时非对映选择性方法利用含有手性助剂的新型中间体。 手性助剂可以是任何手性辅助部分，例如含有取代的恶唑烷酮基团的助剂。 包含手性助剂的中间体在氟化糖的合成中首次使用氟化方法进行氟化，得到氟化中间体，其在除去手性基团后提供所需的关键中间体。 总之，在本发明的方法中，通过手性烯醇化物与亲电氟化剂的反应将氟非对映选择性引入中间体，并且氟化的中间体衍生自甘露醇。