Racemization process of R-zopiclone
    55.
    发明申请
    Racemization process of R-zopiclone 审中-公开
    R-佐匹克隆的外消旋化过程

    公开(公告)号:US20090018336A1

    公开(公告)日:2009-01-15

    申请号:US12215249

    申请日:2008-06-25

    IPC分类号: C07D471/04

    CPC分类号: C07D487/04

    摘要: In one of the embodiments, the present invention provides a racemization process comprising: removing the organic solvent from a mother liquor comprising R-zopiclone malate, eszopiclone malate and an organic solvent to obtain a mixture of R-zopiclone malate and eszopiclone malate; mixing the mixture with water to obtain a solution; neutralizing R-zopiclone malate and eszopiclone malate in the solution to obtain a precipitate of R-zopiclone and eszopiclone; filtering the precipitate; mixing the precipitate of R-zopiclone and eszopiclone with DBU and an organic inert solvent having a boiling point of at least 80° C.; heating; and cooling to obtain a zopiclone racemate.

    摘要翻译: 在一个实施方案中,本发明提供外消旋化方法,其包括:从包含R-佐匹克隆苹果酸酯,苹果酸佐佐匹克和有机溶剂的母液中除去有机溶剂,以获得苹果酸R-佐匹克隆和苹果酸佐佐匹克的混合物; 将混合物与水混合以获得溶液; 在溶液中中和R-佐匹克隆苹果酸盐和右佐剂丙二酸盐,得到R-佐匹克隆和依佐替普的沉淀物; 过滤沉淀物; 将R-佐匹克隆和替佐氟隆的沉淀物与DBU和沸点至少为80℃的有机惰性溶剂混合; 加热; 并冷却以获得佐匹克隆外消旋物。