Processes for the preparation and purification of gabapentin enacarbil
    10.
    发明授权
    Processes for the preparation and purification of gabapentin enacarbil 有权
    加巴喷丁恩卡巴尔的制备和纯化方法

    公开(公告)号:US08283487B2

    公开(公告)日:2012-10-09

    申请号:US12626682

    申请日:2009-11-26

    IPC分类号: C07C271/16

    摘要: Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C10 ether, C2 to C7 ester, C5 to C10 hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula: wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.

    摘要翻译: 从中间体如氨基甲酸1-卤代烷基酯或碳酸酯和二酸缩醛骨架制备和纯化加巴喷丁恩卡巴尔。 例如,通过将C1至C10醇或C1至C10伯胺,选自乙腈,C3至C7酮,C5至C10醚,C2至C7的溶剂组合,制备碳酸1-卤代烷基酯或氨基甲酸酯 酯,C5至C10烃及其组合; 下式的1-卤代烷基卤代甲酸酯:其中每个X独立地选自Br,I或Cl; R1是烷基或H; 和C 6至C 21叔胺。