A process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine hydrochloride (donepezil hcl)
    4.
    发明公开
    A process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine hydrochloride (donepezil hcl) 有权
    Verfahren zur Herstellung von 1-苄基-4 - [(5,6-二甲氧基-1-茚满酮)-2-基]甲基哌啶盐酸盐(多奈哌齐hcl)

    公开(公告)号:EP1531151A1

    公开(公告)日:2005-05-18

    申请号:EP04016772.8

    申请日:2004-07-15

    申请人: USV Limited

    IPC分类号: C07D211/32

    CPC分类号: C07D211/22 C07D211/32

    摘要: This invention describes a process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine hydrochloride (Donepezil HCI) of the formula I
    comprising hydrogenerating 5,6-dimethoxy-2-(pyridin-4-yl)methylene indan-1-one with a noble metal catalyst in a solvent at 20-100°C and 0.7-6.2 bar pressure to form 4-((5,6-dimethoxy-1-indanon)-2-yl)methyl piperidine which is alkylated with an alkylating agent in an organic solvent at 20-80°C.

    摘要翻译: 本发明描述了制备式I的化合物1-(5,6-二甲氧基-1-茚满酮)-2-基甲基哌啶盐酸盐(多奈哌齐HCl)的方法,该方法包括将5,6- 二甲氧基-2-(吡啶-4-基)亚甲基茚满-1-酮与贵金属催化剂在20-100℃和0.7-6.2巴压力下在溶剂中形成4 - ((5,6-二甲氧基-1 - 茚满)-2-基)甲基哌啶,其在有机溶剂中在20-80℃下用烷基化剂烷基化