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    Synthesis of beta-L-2'-deoxy nucleosides
    43.
    发明申请
    Synthesis of beta-L-2'-deoxy nucleosides 审中-公开
    β-L-2'-脱氧核苷的合成

    公开(公告)号：US20050059632A1

    公开(公告)日：2005-03-17

    申请号：US10882893

    申请日：2004-06-30

    申请人： Richard Storer ,  Adel Moussa ,  Jingyang Wang ,  Narayan Chaudhuri ,  Steven Mathieu ,  Alistair Stewart

    发明人： Richard Storer ,  Adel Moussa ,  Jingyang Wang ,  Narayan Chaudhuri ,  Steven Mathieu ,  Alistair Stewart

    IPC分类号： A61K31/7072 ,  A61K31/7076 ,  C07H13/08 ,  C07H19/00 ,  C07H19/048 ,  C07H19/073 ,  C07H19/22 ,  C12Q20060101

    CPC分类号： C07H19/09 ,  C07H9/04 ,  C07H9/06 ,  C07H13/04 ,  C07H13/08 ,  C07H15/203 ,  C07H19/06 ,  C07H19/073 ,  Y02P20/55

    摘要： An improved process for the preparation of 2′-modified nucleosides and 2′-deoxy-nucleosides, such as, β-L-2′-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2′-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2′-anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2′-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2′-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2′-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents.

    摘要翻译： 提供了用于制备2'-修饰的核苷和2'-脱氧核苷的改进方法，例如β-L-2'-脱氧胸苷（LdT）。 特别地，改进的方法涉及可以利用不同起始原料但通过氯糖中间体或通过2,2'-脱水-1-呋喃糖基 - 核碱基中间体进行的2'-脱氧核苷的合成。 当使用2,2'-脱水-1-呋喃糖基碱中间体时，可以使用诸如Red-Al的还原剂和诸如15-冠醚5的多价螯合剂，其引起分子内置换反应和形成 使用所需的产率良好的核苷产物。 本发明的另一种方法是利用不含螯合剂的2,2'-脱水-1-呋喃糖基碱中间产物得到2'-脱氧核苷。 根据本发明制备的化合物可以用作制备其它核苷类似物的中间体，或者可以直接用作抗病毒和/或抗肿瘤剂。

    Imidazopyridayine derivatives having antiviral activity
    45.
    发明授权
    Imidazopyridayine derivatives having antiviral activity 失效
    具有抗病毒活性的咪唑并噻吩衍生物

    公开(公告)号：US4690917A

    公开(公告)日：1987-09-01

    申请号：US800667

    申请日：1985-11-22

    申请人： David J. Knight ,  David I. C. Scopes ,  Richard Storer ,  Stuart Holman

    发明人： David J. Knight ,  David I. C. Scopes ,  Richard Storer ,  Stuart Holman

    IPC分类号： A61K31/50 ,  A61P31/12 ,  C07D487/04 ,  C07D519/00 ,  A61K31/70 ,  C07H3/02

    CPC分类号： C07D487/04 ,  Y02P20/55

    摘要： Compounds of the formula: ##STR1## wherein R.sub.1, R.sub.3 and R.sub.4 each independently represents a hydrogen atom or a protecting group;R.sub.2 represents a halogen atom or a group of formula --NR.sub.a R.sub.b (where R.sub.a and R.sub.b, which may be the same or different, each represents a hydrogen atom or an alkyl group; or R.sub.a and R.sub.b may be linked to form, together with the nitrogen atom to which they are attached, a heterocyclic ring which optionally contains a further heteroatom);and their physiological equivalents as well as salts thereof with acids, exhibit antiviral activity against RNA viruses such as Influenza and/or are intermeidates for the preparation of antivirally active compounds.

    摘要翻译： 下式的化合物：其中R 1，R 3和R 4各自独立地表示氢原子或保护基; R 2表示卤素原子或式-NR a R b的基团（其中R a和R b可以相同或不同，各自表示氢原子或烷基;或者R a和R b可以与 它们所连接的氮原子，任选地含有另外的杂原子的杂环）; 和它们的生理等同物以及其与酸的盐，表现出对RNA病毒如流感的抗病毒活性和/或是用于制备抗病毒活性化合物的中间体。