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    Process for the preparation of indolin-2-one derivatives useful as PR modulators
    3.
    发明申请
    Process for the preparation of indolin-2-one derivatives useful as PR modulators 审中-公开
    制备用作PR调节剂的二氢吲哚-2-酮衍生物的方法

    公开(公告)号：US20080051585A1

    公开(公告)日：2008-02-28

    申请号：US11893335

    申请日：2007-08-15

    申请人： Alexander Gontcharov ,  John Potoski

    发明人： Alexander Gontcharov ,  John Potoski

    IPC分类号： C07D209/04

    CPC分类号： C07D209/96 ,  C07D403/04

    摘要： Processes for dialkylating indolinones, specifically indolin-2-ones are provided. The processes for dialkylating an indolin-2-one include performing the dialkylation in the presence of at least 2 equivalents of a first base, a second base containing at least 1 equivalent of lithium diisopropylamide, and an alkylating agent. Processes for preparing a compound of the structure are provided, wherein R1, R3, R4, R6, R7, R9, and R10 are as defined herein. In one embodiment, a process for preparing 5-(4′-fluoro-2′-oxospiro[cyclopropane-1,3′-indoline]-5′-yl)-1-methyl-1H-pyrrole-2-carbonitrile is provided.

    摘要翻译： 提供二氢化吲哚啉酮，特别是二氢吲哚-2-酮的方法。 使二氢化茚-2-酮二烷基化的方法包括在至少2当量的第一碱，含有至少1当量二异丙基氨基锂的烷基化剂和烷基化剂的存在下进行二烷基化。 提供了制备结构化合物的方法，其中R 1，R 3，R 4，R 6， >，R 7，R 9和R 10如本文所定义。 在一个实施方案中，提供了制备5-（4'-氟-2'-氧代螺[环丙烷-1,3'-二氢吲哚] -5'-基）-1-甲基-1H-吡咯-2-甲腈的方法 。

    PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS
    6.
    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。