Process for the preparation of aripiprazole
    1.
    发明申请
    Process for the preparation of aripiprazole 失效
    制备阿立哌唑的方法

    公开(公告)号:US20060258869A1

    公开(公告)日:2006-11-16

    申请号:US11448504

    申请日:2006-06-07

    IPC分类号: C07D215/02 C07D215/00

    CPC分类号: C07D215/227

    摘要: The present invention relates to an improved process for the preparation of 7-[4[-(2,3-dichlorophenyl) -1-piperazinyl]butoxy]3,4-dihydro-2-(1H) quinolinone (Aripiprazole) having dimer impurity less than 0.15%, particularly, the present invention relates to an improved process for the preparation of 7-(4-chlorobutoxy)-3,4-dihydrocarbostyril of formula (I) having dimer impurity less than 0.5% comprising a step of, reacting 7-hydroxy-tetrahydroquinolinone of formula (III) with 1-bromo-4-chlorobutane in the presence of a base in a solvent.

    摘要翻译: 本发明涉及制备具有二聚体杂质的7- [4 - [(2,3-二氯苯基)-1-哌嗪基]丁氧基] 3,4-二氢-2-(1H)喹啉酮(阿立哌唑)的改进方法 小于0.15%,特别是本发明涉及制备具有二聚体杂质小于0.5%的式(I)的7-(4-氯丁氧基)-3,4-二氢喹诺酮的改进方法,包括以下步骤:使 (III)的7-羟基 - 四氢喹啉酮与1-溴-4-氯丁烷在碱存在下在溶剂中反应。