利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

30 条记录 (耗时 0.032 秒)

    PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS
    4.
    发明申请
    PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS 审中-公开
    合成前列腺素受体调节剂的方法

    公开(公告)号：US20080319204A1

    公开(公告)日：2008-12-25

    申请号：US12120959

    申请日：2008-05-15

    申请人： Yanzhong Wu ,  Karen Sutherland ,  John Leo Considine ,  Bogdan Kazimierz Wilk ,  Pierre Giguere ,  Michael MacEwan ,  Archana Sharma ,  Alexander Gontcharov

    发明人： Yanzhong Wu ,  Karen Sutherland ,  John Leo Considine ,  Bogdan Kazimierz Wilk ,  Pierre Giguere ,  Michael MacEwan ,  Archana Sharma ,  Alexander Gontcharov

    IPC分类号： C07D209/96

    CPC分类号： C07D209/96 ,  C07D403/04

    摘要： Processes for preparing substituted oxindole-2-ones, and specifically the following, are described, wherein R1-R4, R6, and n are defined herein. The processes include reacting a first alkali metal hydroxide, a tetraalkyl ammonium salt, a benzonitrile, and R6X or XCH2(CH2)nX′, wherein R6 is C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, or substituted heterocyclic, X and X′ are, independently, leaving groups, and n is 1 to 5; (ii) reacting the product of step (i) with a second alkali metal hydroxide at a temperature of at least about 60° C.; (iii) reacting the product of step (ii) with an alkali alkoxide at a temperature of at least about 140° C. to form an oxindol-2-one; (iv) brominating the oxindol-2-one; and (v) coupling the brominated oxindol-2-one with a coupling reagent.

    摘要翻译： 描述了制备取代羟吲哚-2-酮的方法，具体如下，其中R1-R4，R6和n如本文所定义。 所述方法包括使第一碱金属氢氧化物，四烷基铵盐，苄腈和R6X或XCH2（CH2）nX'反应，其中R6为C1至C6烷基，取代的C1至C6烷基，C3至C8环烷基，取代C3至 C8环烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，杂环或取代的杂环，X和X'独立地为离去基团，n为1至5; （ii）使步骤（i）的产物与至少约60℃的温度下的第二碱金属氢氧化物反应; （iii）使步骤（ii）的产物与碱金属醇盐在至少约140℃的温度下反应，形成羟吲哚-2-酮; （iv）溴化羟吲哚-2-酮; 和（v）将溴代羟吲哚-2-酮与偶联剂偶联。

    Advanced route for the synthesis of cPLA2 inhibitors
    8.
    发明申请
    Advanced route for the synthesis of cPLA2 inhibitors 失效
    用于合成cPLA2抑制剂的先进途径

    公开(公告)号：US20050020858A1

    公开(公告)日：2005-01-27

    申请号：US10896318

    申请日：2004-07-21

    申请人： Yanzhong Wu ,  Panolil Raveendranath

    发明人： Yanzhong Wu ,  Panolil Raveendranath

    IPC分类号： C07C303/38 ,  C07C303/40 ,  C07C311/03 ,  C07C311/05 ,  C07C311/13 ,  C07D209/14

    CPC分类号： C07C303/38 ,  C07C303/40 ,  C07C311/13 ,  C07D209/14

    摘要： A process for making a compound of formula (I) in which process the compound HC≡C—(CH2)n—NH2 is reacted with the compound R1—SO2Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formula to produce the compound of formula (I), and compounds produced by the process of this invention. The terms R1, R2, R3, R4 and n have the definitions set forth in the specification.

    摘要翻译： 制备其中化合物HC = C-（CH 2）n -NH 2的方法与化合物R1-SO2Cl反应以制备中间体化合物的式（I）化合物的方法，然后将该中间体化合物与 制备式（I）化合物的方案，以及通过本发明方法制备的化合物。 术语R1，R2，R3，R4和n具有说​​明书中阐述的定义。