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5 条记录 (耗时 0.009 秒)

    PROCESS AND INTERMEDIATES FOR PRODUCTION OF DONEPEZIL AND RELATED COMPOUNDS
    2.
    发明公开
    PROCESS AND INTERMEDIATES FOR PRODUCTION OF DONEPEZIL AND RELATED COMPOUNDS 审中-公开
    过程和中间产品用于制备多奈哌齐及相关化合物

    公开(公告)号：EP1129073A2

    公开(公告)日：2001-09-05

    申请号：EP99936948.1

    申请日：1999-08-11

    申请人： Finetech Ltd

    发明人： GUTMAN, L., Arie ,  SHKOLNIK, Eleonora ,  TISHIN, Boris ,  NISNEVICH, Genady ,  ZALTZMAN, Igor

    IPC分类号： C07D211/32 ,  C07D211/34

    CPC分类号： C07D211/32 ,  C07D211/34

    摘要： The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R1 is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; 4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-(φ-aralkyl)-4-piperidyl; 4-pyridyl; R?4, R5, R6 and R7¿ are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4 or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R?1, R4, R5, R6 and R7¿, m and n are as defined above; R2 is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R3 is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents. One of the most potent acetylcholinesterase inhibitors of the class of compounds prepared according to the present invention is donepezil.

    PROCESS AND A NOVEL INTERMEDIATE FOR THE PREPARATION OF FLECAINIDE
    3.
    发明公开
    PROCESS AND A NOVEL INTERMEDIATE FOR THE PREPARATION OF FLECAINIDE 失效
    用于生产中间氟卡尼在此过程中

    公开(公告)号：EP0996616A1

    公开(公告)日：2000-05-03

    申请号：EP98931000.8

    申请日：1998-07-07

    申请人： Finetech Ltd

    发明人： GUTMAN, Arie, L. ,  NISNEVICH, Genady ,  SHKOLNIK, Eleonora ,  ZALTZMAN, Igor

    IPC分类号： C07D213/40 ,  C07D211/26 ,  C07C255/14 ,  C07B43/06

    CPC分类号： C07D213/40 ,  C07C255/14 ,  C07D211/26

    摘要： The present invention provides a process for the preparation of a compound of formula (A) wherein R is a 2-piperidyl or 2-pyridyl radical, and pharmaceutically acceptable salts thereof, which process comprises the steps of: a) reacting 2,5 bis (2,2,2,-trifluoroethoxy) benzoic acid or a salt thereof, with a haloacetonitrile of the formula XCH2CN, where X is C1, Br or I, if necessary in the presence of an inorganic or organic base, to form the cyanomethyl ester of formula (II); b) reacting the ester of formula (II) with an amine of the formula RCH2NH2, where R is as defined above and, if desired; c) converting the compound of the formula (A) to a pharmaceutically acceptable salt thereof.

    PROCESS AND A NOVEL INTERMEDIATE FOR THE PREPARATION OF FLECAINIDE
    4.
    发明授权
    PROCESS AND A NOVEL INTERMEDIATE FOR THE PREPARATION OF FLECAINIDE 失效
    用于生产中间氟卡尼在此过程中

    公开(公告)号：EP0996616B1

    公开(公告)日：2004-05-12

    申请号：EP98931000.8

    申请日：1998-07-07

    申请人： Finetech Ltd

    发明人： GUTMAN, Arie, L. ,  NISNEVICH, Genady ,  SHKOLNIK, Eleonora ,  ZALTZMAN, Igor

    IPC分类号： C07D213/40 ,  C07D211/26 ,  C07C255/14 ,  C07B43/06

    CPC分类号： C07D213/40 ,  C07C255/14 ,  C07D211/26

    摘要： The present invention provides a process for the preparation of a compound of formula (A) wherein R is a 2-piperidyl or 2-pyridyl radical, and pharmaceutically acceptable salts thereof, which process comprises the steps of: a) reacting 2,5 bis (2,2,2,-trifluoroethoxy) benzoic acid or a salt thereof, with a haloacetonitrile of the formula XCH2CN, where X is C1, Br or I, if necessary in the presence of an inorganic or organic base, to form the cyanomethyl ester of formula (II); b) reacting the ester of formula (II) with an amine of the formula RCH2NH2, where R is as defined above and, if desired; c) converting the compound of the formula (A) to a pharmaceutically acceptable salt thereof.