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    Enantioselective synthesis of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-JK][1]-benzazepin-2[1H]-one and zilpaterol
    1.
    发明申请
    Enantioselective synthesis of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-JK][1]-benzazepin-2[1H]-one and zilpaterol 有权
    6-氨基-7-羟基-4,5,6,7-四氢 - 咪唑并[4,5,1-JK] [1] - 苯并氮杂-2 [1H] - 酮和齐帕特罗的对映选择性合成

    公开(公告)号：US20100173892A1

    公开(公告)日：2010-07-08

    申请号：US12525222

    申请日：2008-01-31

    申请人： Juan Jose Almena-Perea ,  Monika Brink ,  Gerhard Geiss ,  Renat Kadyrov ,  Thorsten Meyer

    发明人： Juan Jose Almena-Perea ,  Monika Brink ,  Gerhard Geiss ,  Renat Kadyrov ,  Thorsten Meyer

    IPC分类号： A61K31/55 ,  C07D487/06 ,  A61P3/00

    CPC分类号： C07D487/06

    摘要： This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6, 7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.

    摘要翻译： 本发明涉及一种用于氢化酮肟以选择性形成氨基醇立体异构体的方法，特别涉及氢化4,5-二氢 - 咪唑并[4,5,1-jk] [1] 苯并吖庚因-2,6,7 [1H] - 三酮-6-肟或其盐，以选择性地形成6-氨基-7-羟基-4,5,6,7-四氢 - 咪唑并[4,5,5- 1-jk] [1] - 苯并氮杂-2 [1H] - 酮或其盐。 本发明还涉及6-氨基-7-羟基-4,5,6,7-四氢 - 咪唑并[4,5,1-jk] [1] - 苯并氮杂-2 [1H] - 酮氢化物 产物或其盐选择性地制备齐勒特罗或其盐的立体异构体，以及在治疗方法和动物药物中使用这种齐伐他醇立体异构体或盐。