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    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。

    Process for preparation of 4-amino-3-quinolinecarbonitriles
    7.
    发明申请
    Process for preparation of 4-amino-3-quinolinecarbonitriles 失效
    制备4-氨基-3-喹啉碳腈的方法

    公开(公告)号：US20050043537A1

    公开(公告)日：2005-02-24

    申请号：US10918947

    申请日：2004-08-16

    申请人： Karen Sutherland ,  Gregg Feigelson ,  Diane Boschelli ,  David Blum ,  Henry Strong

    发明人： Karen Sutherland ,  Gregg Feigelson ,  Diane Boschelli ,  David Blum ,  Henry Strong

    IPC分类号： C07D215/54 ,  C07D405/04 ,  C07D495/04 ,  C07D215/38

    CPC分类号： C07D405/04 ,  C07D215/54 ,  C07D495/04

    摘要： This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

    摘要翻译： 本发明公开了一种制备4-氨基-3-喹啉甲腈的方法，包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺在醇溶剂和三烷基原甲酸酯中缩合，得到3-氨基-2-氰基丙烯酰胺; 任选在催化剂存在下，将3-氨基-2-氰基丙烯酰胺与三氯氧化磷在乙腈，丁腈，甲苯或二甲苯中的混合，得到4-氨基-3-喹啉腈，并公开了制备7-氨基-2-氰基丙烯酰胺的方法， 氨基 - 噻吩并[3,2-b]吡啶-6-甲腈，其包括在醇溶剂中组合二取代的3-氨基噻吩与氰基乙酰胺和三烷基酯，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈，丁腈，甲苯或二甲苯组合，任选在催化剂存在下，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和 还公开了通过将胺化合物与氰基乙酸和肽偶联剂组合以制备悬浮液来制备4-氨基-3-喹啉腈的方法; 过滤悬浮液，得到氰基乙酰胺; 将氰基乙酰胺与任选的高达四取代的苯胺，醇溶剂和原甲酸三乙酯缩合，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯组合，得到4-氨基-3-喹啉腈。

    Process for preparation of 4-amino-3-quinolinecarbonitriles
    10.
    发明申请
    Process for preparation of 4-amino-3-quinolinecarbonitriles 审中-公开
    制备4-氨基-3-喹啉碳腈的方法

    公开(公告)号：US20080033175A1

    公开(公告)日：2008-02-07

    申请号：US11973259

    申请日：2007-10-05

    申请人： Karen Sutherland ,  Gregg Feigelson ,  Diane Boschelli ,  David Blum ,  Henry Strong

    发明人： Karen Sutherland ,  Gregg Feigelson ,  Diane Boschelli ,  David Blum ,  Henry Strong

    IPC分类号： C07D401/00 ,  C07D471/02

    CPC分类号： C07D405/04 ,  C07D215/54 ,  C07D495/04

    摘要： This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

    摘要翻译： 本发明公开了一种制备4-氨基-3-喹啉甲腈的方法，包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺在醇溶剂和三烷基原甲酸酯中缩合，得到3-氨基-2-氰基丙烯酰胺; 任选在催化剂存在下，将3-氨基-2-氰基丙烯酰胺与三氯氧化磷在乙腈，丁腈，甲苯或二甲苯中的混合，得到4-氨基-3-喹啉腈，并公开了制备7-氨基-2-氰基丙烯酰胺的方法， 氨基 - 噻吩并[3,2-b]吡啶-6-甲腈，其包括在醇溶剂中组合二取代的3-氨基噻吩与氰基乙酰胺和三烷基酯，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈，丁腈，甲苯或二甲苯组合，任选在催化剂存在下，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和 还公开了通过将胺化合物与氰基乙酸和肽偶联剂组合以制备悬浮液来制备4-氨基-3-喹啉腈的方法; 过滤悬浮液，得到氰基乙酰胺; 将氰基乙酰胺与任选的高达四取代的苯胺，醇溶剂和原甲酸三乙酯缩合，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯组合，得到4-氨基-3-喹啉腈。