Method For Producing Azoniaspironortropine Esters And Nortropan-3-One Compounds
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    发明申请
    Method For Producing Azoniaspironortropine Esters And Nortropan-3-One Compounds 审中-公开
    方法生产Azoniaspironortropine酯和Nortropan-3-One化合物

    公开(公告)号:US20100048903A1

    公开(公告)日:2010-02-25

    申请号:US12543193

    申请日:2009-08-18

    IPC分类号: C07D451/00 C07D451/02

    CPC分类号: C07D451/06 C07D451/10

    摘要: The present technology relates to an improved one-stage method for producing azoniaspironortropine esters such as trospium chloride by reacting an endonortropine compound with an organic dihalogen compound and an a-hydroxycarboxylic acid in the presence of a base and 1,1′ carbonyldiimidazole or 1,1′ thiocarbonyldiimidazole or thionyldiimidazole. The present technology also relates to an improved method for producing nortropan-3-one compounds or their hydrohalides (such as N-benzyltropanone hydrochloride) by reacting an amine and a protected dialdehyde with a basic aqueous solution of 1,3-acetone dicarboxylic acid.

    摘要翻译: 本技术涉及通过在碱和1,1'羰基二咪唑或1'羰基二咪唑存在下,使内皮质素化合物与有机二卤素化合物和α-羟基羧酸反应来制备氮杂索罗丹司酸酯例如氯化梭罗的改进的一步法, 1'硫代羰基二咪唑或亚硫酰二咪唑。 本技术还涉及通过使胺和被保护的二醛与碱式1,3-丙二醇二羧酸水溶液反应来生产异丙肾上腺素-3-酮化合物或其氢卤酸盐(例如N-苄基丙酰氯盐酸盐)的改进方法。