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    PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS
    2.
    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。

    Process for the preparation of tubulin inhibitors
    6.
    发明授权
    Process for the preparation of tubulin inhibitors 失效
    微管蛋白抑制剂的制备方法

    公开(公告)号：US07396835B2

    公开(公告)日：2008-07-08

    申请号：US11007839

    申请日：2004-12-08

    申请人： Yanzhong Wu ,  Jean Schmid ,  Jay Thomas Afragola ,  David Blum ,  Semiramis Ayral-Kaloustian

    发明人： Yanzhong Wu ,  Jean Schmid ,  Jay Thomas Afragola ,  David Blum ,  Semiramis Ayral-Kaloustian

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention provides a process for the preparation of 6-[(substituted)phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R1 is CF3 or C2F5; R2 is H or C1-C3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R3 and R4 are each independently H or C1-C3 alkyl; or R3 and R4 when optionally taken together with the nitrogen atom to which each is attached form a 4 to 6 membered saturated heterocyclic ring having 1-2 nitrogen atoms and 0-1 oxygen atoms or 0-1 sulfur atoms, and optionally substituted with R5; R5 is C1-C3 alkyl; wherein the dotted line is an optional bond.

    摘要翻译： 本发明提供了制备6 - [（取代的）苯基] - 三唑并嘧啶二羧酸盐和具有结构式（I）的水合盐的方法，其中：R 1是CF 3 或C 2 F 5; R 2是H或C 1 -C 3烷基; n是2,3或4的整数; X是Cl或Br; R 3和R 4各自独立地为H或C 1 -C 3烷基; 或R 3和R 4当任选地与各自连接的氮原子一起形成具有1-2个氮原子的4至6元饱和杂环和0 -1个氧原子或0-1个硫原子，并且任选被R 5取代; R 5是C 1 -C 3烷基; R 5是C 1 -C 3烷基; 其中虚线是任选的键。

    Process for the preparation of tubulin inhibitors
    8.
    发明申请
    Process for the preparation of tubulin inhibitors 失效
    微管蛋白抑制剂的制备方法

    公开(公告)号：US20050124635A1

    公开(公告)日：2005-06-09

    申请号：US11007839

    申请日：2004-12-08

    申请人： Yanzhong Wu ,  Jean Schmid ,  Jay Afragola ,  David Blum ,  Semiramis Ayral-Kaloustian

    发明人： Yanzhong Wu ,  Jean Schmid ,  Jay Afragola ,  David Blum ,  Semiramis Ayral-Kaloustian

    IPC分类号： C07D487/04 ,  A61K31/519

    CPC分类号： C07D487/04

    摘要： The present invention provides a process for the preparation of 6-[(substituted)phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R1 is CF3 or C2F5; R2 is H or C1-C3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R3 and R4 are each independently H or C1-C3 alkyl; or R3 and R4 when optionally taken together with the nitrogen atom to which each is attached form a 4 to 6 membered saturated heterocyclic ring having 1-2 nitrogen atoms and 0-1 oxygen atoms or 0-1 sulfur atoms, and optionally substituted with R5; R5 is C1-C3 alkyl; wherein the dotted line is an optional bond.

    摘要翻译： 本发明提供了制备6 - [（取代的）苯基] - 三唑并嘧啶二羧酸盐和具有结构式（I）的水合盐的方法，其中：R 1是CF 3 或C 2 F 5; R 2是H或C 1 -C 3烷基; n是2,3或4的整数; X是Cl或Br; R 3和R 4各自独立地为H或C 1 -C 3烷基; 或R 3和R 4当任选地与各自连接的氮原子一起形成具有1-2个氮原子的4至6元饱和杂环和0 -1个氧原子或0-1个硫原子，并且任选被R 5取代; R 5是C 1 -C 3烷基; R 5是C 1 -C 3烷基; 其中虚线是任选的键。