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    Process for the preparation of indole derivatives
    16.
    发明申请
    Process for the preparation of indole derivatives 审中-公开
    吲哚衍生物的制备方法

    公开(公告)号：US20050032875A1

    公开(公告)日：2005-02-10

    申请号：US10487269

    申请日：2002-08-13

    申请人： Heinz Wolleb ,  Annemarie Wolleb ,  Paul Van Der Schaaf ,  Roman Kolly ,  Nicole End

    发明人： Heinz Wolleb ,  Annemarie Wolleb ,  Paul Van Der Schaaf ,  Roman Kolly ,  Nicole End

    IPC分类号： C07D209/12 ,  B01J31/18 ,  B01J31/24 ,  C07D209/24 ,  C07D319/06 ,  C07D405/06 ,  C07F5/02 ,  A61K31/405

    CPC分类号： C07D405/06 ,  C07D209/24 ,  C07D319/06 ,  C07F5/025 ,  Y02P20/55

    摘要： A process for the preparation of compounds of formula (I) wherein R1 is unsubstituted or substituted C1-C8alkyl, R2, R3, R4 and R5 are each independently of the others hydrogen, unsubstituted or substituted C1-C8alkyl, C1-C8 alkoxy, phenoxy or benzyloxy, or halogen, Y1 and Y2 are each independently of the other hydrogen or a protecting group, or Y1 and Y2 together form a protecting bridge, and X1 is hydrogen, an organic radical or a cation, in which process a compound of formula (II) wherein R1 R2, R3, R4 and R5 are as defined above and Z1 is a leaving group, is reacted, in the presence of a catalytically effective amount of a palladium catalyst, with a compound of formula (III) wherein R6 is hydrogen, bromine, chlorine, iodine, —OSO2CF3, —COCI, —B(OH)2 or a mono- or di-ester derived from —B(OH)2, Y3 and Y4 are each a protecting group, or Y3 and Y4 together form a protecting bridge, and X1 is as defined above, to form a compound of formula (IV) and if desired the radicals Y3 and Y4 are converted into the radicals Y1 and Y2 where Y1 and Y2 are hydrogen.

    摘要翻译： 制备其中R 1为未取代或取代的C 1 -C 8烷基，R 2，R 3，R 4和R 5的式（I）化合物的方法各自独立地为氢，未取代或取代的C 1 -C 8烷基，C 1 -C 8烷氧基，苯氧基 或苄氧基或卤素，Y1和Y2各自独立地为另一个氢或保护基，或Y1和Y2一起形成保护桥，并且X 1是氢，有机基团或阳离子，其中式 （II）其中R1 R2，R3，R4和R5如上定义，Z1是离去基团，在催化有效量的钯催化剂存在下，与式（III）化合物反应，其中R 6是 氢，溴，氯，碘，-OSO 2 CF 3，-COCI，-B（OH）2或衍生自-B（OH）2，Y 3和Y 4的单酯或二酯各自为保护基，或Y 3和Y 4 一起形成保护桥，X1如上所定义，形成式（IV）的化合物，如果需要，基团Y 3和Y 4是 转化为Y1和Y2基团，其中Y1和Y2是氢。