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    PROCESS FOR OBTAINING ENANTIOMERS OF DULOXETINE PRECURSORS
    9.
    发明申请
    PROCESS FOR OBTAINING ENANTIOMERS OF DULOXETINE PRECURSORS 审中-公开
    获得杜鹃素前体成分的方法

    公开(公告)号：US20090247771A1

    公开(公告)日：2009-10-01

    申请号：US12280084

    申请日：2007-02-27

    申请人： Helmut Heinrich Buschmann ,  Antoni Torrens Jover ,  Matthias Lormann ,  Stefan Dahmen

    发明人： Helmut Heinrich Buschmann ,  Antoni Torrens Jover ,  Matthias Lormann ,  Stefan Dahmen

    IPC分类号： C07D333/16

    CPC分类号： C07D333/24 ,  C07D333/12 ,  C07D333/14 ,  Y02P20/55

    摘要： The present invention is directed to a process for the preparation of an enantiomerically enriched compound of formula II wherein, R1, R2 and R3 are each independently selected from hydrogen, halogen, substituted or unsubstituted lower alkyl or substituted or unsubstituted aryl; X is —C(═O)-Z or —Y, wherein —Y is selected from —CH2—OR4, —CH2-halogen or —CH2—NR6R7; wherein Z is selected from —NR6R7 or —OR5, wherein R5 is selected from hydrogen, substituted or unsubstituted lower alkyl or ester activating group; R4 is selected from hydrogen, hydroxyl protecting group or hydroxyl activating group; R6 and R7 are each independently selected from hydrogen, amino protecting group, amido protecting group or substituted or unsubstituted lower alkyl; or a pharmaceutically acceptable salt, complex or solvate thereof; which comprises an enantioselective addition with a thienyl zinc reagent, in the presence of a chiral ligand.

    摘要翻译： 本发明涉及制备对映体富集的式II化合物的方法，其中R 1，R 2和R 3各自独立地选自氢，卤素，取代或未取代的低级烷基或取代或未取代的芳基; X是-C（-O）-Z或-Y，其中-Y选自-CH2-OR4，-CH2-卤素或-CH2-NR6R7; 其中Z选自-NR 6 R 7或-OR 5，其中R 5选自氢，取代或未取代的低级烷基或酯活化基团; R4选自氢，羟基保护基或羟基活化基团; R6和R7各自独立地选自氢，氨基保护基，酰氨基保护基或取代或未取代的低级烷基; 或其药学上可接受的盐，复合物或溶剂化物; 其包括在手性配体存在下用噻吩锌试剂进行对映选择性加成。