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36 条记录 (耗时 0.039 秒)

    Asymmetric synthesis of R and S warfarin and its analogs
    1.
    发明授权
    Asymmetric synthesis of R and S warfarin and its analogs 失效
    R和S华法林及其类似物的不对称合成

    公开(公告)号：US5686631A

    公开(公告)日：1997-11-11

    申请号：US678211

    申请日：1996-07-11

    申请人： Hui-Yin Li ,  Andrea Jane Robinson

    发明人： Hui-Yin Li ,  Andrea Jane Robinson

    IPC分类号： C07D20060101 ,  C07D311/56 ,  C07D311/02

    CPC分类号： C07D311/56

    摘要： The present invention provides a novel process for making compounds of formula 2a or 2b or pharmaceutically acceptable salts thereof, ##STR1## wherein R1 is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO.sub.2 and halogen; R.sub.2 is H; R.sub.3 is selected from the group consisting of C.sub.1-4 alkyl, phenyl, and benzyl; and, R.sub.4 is selected from the group consisting of H and halogen; which comprises the steps of: a) oxidizing a racemate of formula 2 or a salt thereof to form a dehydro-compound of formula 3, ##STR2## wherein R.sub.5 is selected from the group consisting of H, CH.sub.3, benzyl, C.sub.2-8 acyl Na, Li and K; and, b) asymmetrically hydrogenating a compound of formula 3 in the presence of a chiral phosphine catalyst to form a compound of formula 2a or 2b.

    摘要翻译： 本发明提供制备式2a或2b化合物或其药学上可接受的盐的新方法，其中R 1选自苯基和至少被取代的苯基 一个选自NO2和卤素的基团; R2为H; R 3选自C 1-4烷基，苯基和苄基; 并且R 4选自H和卤素; 其包括以下步骤：a）氧化式2的外消旋物或其盐以形成式3的脱氢化合物，其中H，CH 3，苄基，C 2-8酰基Na，Li和K ; 和b）在手性膦催化剂的存在下不对称地氢化式3的化合物以形成式2a或2b的化合物。

    Asymmetric R and S warfarin and its analogs
    2.
    发明授权
    Asymmetric R and S warfarin and its analogs 失效
    不对称R和S华法林及其类似物

    公开(公告)号：US5856525A

    公开(公告)日：1999-01-05

    申请号：US950018

    申请日：1997-10-14

    申请人： Hui-Yin Li ,  Andrea Jane Robinson

    发明人： Hui-Yin Li ,  Andrea Jane Robinson

    IPC分类号： C07D20060101 ,  C07D311/56 ,  C07D311/02

    CPC分类号： C07D311/56

    摘要： The present invention provides a novel process for making compounds of formula 2a or 2b or pharmaceutically acceptable salts thereof, ##STR1## wherein R.sub.1 is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO.sub.2 and halogen;R.sub.2 is H;R.sub.3 is selected from the group consisting of C.sub.1-4 alkyl, phenyl, and benzyl; and,R.sub.4 is selected from the group consisting of H and halogen;which comprises the steps of:a) oxidizing a racemate of formula 2 or a salt thereof to form a dehydro-compound of formula 3, ##STR2## wherein R.sub.5 is selected from the group consisting of H, CH.sub.3, benzyl, C.sub.2-8 acyl Na, Li and K; and,b) asymmetrically hydrogenating a compound of formula 3 in the presence of a chiral phosphine catalyst to form a compound of formula 2a or 2b.

    摘要翻译： 本发明提供制备式2a或2b化合物或其药学上可接受的盐的新方法，其中R 1选自苯基和至少被取代的苯基 一个选自NO2和卤素的基团; R2为H; R 3选自C 1-4烷基，苯基和苄基; 并且R 4选自H和卤素; 其包括以下步骤：a）氧化式2的外消旋物或其盐以形成式3的脱氢化合物，由H，CH 3，苄基，C 2-8酰基Na，Li和K组成的图像 ; 和b）在手性膦催化剂的存在下不对称地氢化式3的化合物以形成式2a或2b的化合物。

    SYNTHESIS AND USE OF KINASE INHIBITORS
    4.
    发明申请
    SYNTHESIS AND USE OF KINASE INHIBITORS 有权
    合成和使用激酶抑制剂

    公开(公告)号：US20140235635A1

    公开(公告)日：2014-08-21

    申请号：US13961517

    申请日：2013-08-07

    申请人： Yixiong Lei ,  Carl Henry Behrens ,  Hui-Yin Li ,  Connie L. Sun

    发明人： Yixiong Lei ,  Carl Henry Behrens ,  Hui-Yin Li ,  Connie L. Sun

    IPC分类号： C07D213/74

    CPC分类号： C07D213/74 ,  C07D279/10 ,  C07D413/12

    摘要： An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.

    摘要翻译： 提供了一类改进的焦点粘附激酶（FAK）抑制剂的合成，其中降低了昂贵的钯基催化剂的使用，提高了反应产率和产品纯度。 芳基卤化物与苯胺的偶联的两个关键反应被优化，令人惊奇的发现是可以完全在一个反应​​中分配钯基催化剂。 本发明还提供了FAK抑制化合物在治疗炎症和免疫疾病和关节炎中的用途。