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    Process for preparing a piperidine derivative
    3.
    发明授权
    Process for preparing a piperidine derivative 失效
    哌啶衍生物的制备方法

    公开(公告)号：US06610851B1

    公开(公告)日：2003-08-26

    申请号：US09695383

    申请日：2000-10-25

    申请人： Kiyoshi Sugi ,  Nobushige Itaya ,  Tadashi Katsura ,  Masami Igi ,  Shigeya Yamazaki ,  Taro Ishibashi ,  Teiji Yamaoka ,  Yoshihiro Kawada ,  Yayoi Tagami

    发明人： Kiyoshi Sugi ,  Nobushige Itaya ,  Tadashi Katsura ,  Masami Igi ,  Shigeya Yamazaki ,  Taro Ishibashi ,  Teiji Yamaoka ,  Yoshihiro Kawada ,  Yayoi Tagami

    IPC分类号： C07D40512

    CPC分类号： C07D405/12 ,  C07D211/22 ,  C07D211/60 ,  C07D211/76

    摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is carbonyl group, then R2 is carboxyl group or —CO2R7 group (R7 is as defined above); or (C) when R1 is hydrogen atom and Z is methylene group, then R2 is hydroxymethyl group.

    摘要翻译： 哌啶衍生物，其可以用作药物的中间体，例如用作抗抑郁药的帕罗西汀，由通式（I）表示：其中R1是氢原子，苄氧基羰基或叔丁氧基羰基; R2是羟甲基，具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基，4-位可具有甲基的苯基磺酰氧基甲基，（3,4-亚甲二氧基苯基）氧甲基，羧基或-CO 2 R 7基，其中 R7为碳原子数为1〜5的烷基，Z为亚甲基或羰基，条件是（A）当R1为苄氧羰基或叔丁氧基羰基时，则R2为羟甲基，烷基磺酰氧基甲基为 具有1至2个碳原子的烷基部分，可以在4-位具有甲基的苯基磺酰氧基甲基或（3,4-亚甲二氧基苯基）氧基甲基，Z是亚甲基; 或（B）当R 1为氢原子且Z为羰基时，则R 2为羧基或-CO 2 R 7基（R 7如上所定义）; 或（C）当R 1为氢原子且Z为亚甲基时，则R 2为羟甲基。

    Piperidine derivative and process for preparing the same
    4.
    发明授权
    Piperidine derivative and process for preparing the same 失效
    哌啶衍生物及其制备方法

    公开(公告)号：US06476227B1

    公开(公告)日：2002-11-05

    申请号：US09550175

    申请日：2000-04-14

    申请人： Kiyoshi Sugi ,  Nobushige Itaya ,  Tadashi Katsura ,  Masami Igi ,  Shigeya Yamazaki ,  Taro Ishibashi ,  Teiji Yamaoka ,  Yoshihiro Kawada ,  Yayoi Tagami

    发明人： Kiyoshi Sugi ,  Nobushige Itaya ,  Tadashi Katsura ,  Masami Igi ,  Shigeya Yamazaki ,  Taro Ishibashi ,  Teiji Yamaoka ,  Yoshihiro Kawada ,  Yayoi Tagami

    IPC分类号： C07D21140

    CPC分类号： C07D405/12 ,  C07D211/22 ,  C07D211/60 ,  C07D211/76

    摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is carbonyl group, then R2 is carboxyl group or —CO2R7 group (R7 is as defined above); or (C) when R1 is hydrogen atom and Z is methylene group, then R2 is hydroxymethyl group.

    摘要翻译： 哌啶衍生物，其可以用作药物的中间体，例如用作抗抑郁药的帕罗西汀，由通式（I）表示：其中R1是氢原子，苄氧基羰基或叔丁氧基羰基; R2是羟甲基，具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基，4-位可具有甲基的苯基磺酰氧基甲基，（3,4-亚甲二氧基苯基）氧甲基，羧基或-CO 2 R 7基，其中 R7为碳原子数为1〜5的烷基，Z为亚甲基或羰基，条件是（A）当R1为苄氧羰基或叔丁氧基羰基时，则R2为羟甲基，烷基磺酰氧基甲基为 具有1至2个碳原子的烷基部分，可以在4-位具有甲基的苯基磺酰氧基甲基或（3,4-亚甲二氧基苯基）氧基甲基，Z是亚甲基; 或（B）当R 1为氢原子且Z为羰基时，则R 2为羧基或-CO 2 R 7基（R 7如上所定义）; 或（C）当R 1为氢原子且Z为亚甲基时，则R 2为羟甲基。