Piperidine derivative as intermediates for the preparation of paroxetine and process for their preparation
    87.
    发明公开
    Piperidine derivative as intermediates for the preparation of paroxetine and process for their preparation 失效
    哌啶衍生物作为中间体用于帕罗西汀的制备和它们的制备方法

    公开(公告)号:EP0812827A1

    公开(公告)日:1997-12-17

    申请号:EP97303647.8

    申请日:1997-05-29

    IPC分类号: C07D211/22

    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 R 1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R 2 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 -CO 2 R 7 group in which R 7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R 1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R 2 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 R 1 is hydrogen atom and Z is carbonyl group, then R 2 is carboxyl group or -CO 2 R 7 group (R 7 is as defined above); or (C) when R 1 is hydrogen atom and Z is methylene group, then R 2 is hydroxymethyl group.
    Also processes for the production of the intermediates are described.

    摘要翻译: 的哌啶衍生物,它可以用作医药中间体到:如帕罗西汀作为抗抑郁药是有用的,由通式(I)表示: worin - [R <1>是氢原子,苄氧羰基或叔丁氧基羰基; [R <2>是羟甲基,以alkylsulfonyloxymethyl具有的1至2个碳原子,phenylsulfonyloxymethyl基,它们可在4位上具有甲基,(3,4-亚甲二氧苯基)氧甲基,羧基或-CO 2烷基部分基 <7>团,其中R <7>是具有1至5个碳原子的烷基,且Z是亚甲基或羰基,条件是,(A)当R <1>是苄氧羰基或叔丁氧基羰基 ,则成为<2>是羟甲基,具有1〜2个碳原子,phenylsulfonyloxymethyl基,它们可在4位或(3,4-亚甲二氧苯基)氧甲基组具有甲基烷基部分到alkylsulfonyloxymethyl基团,Z是 亚甲基; 或(B)当R <1>是氢原子,Z为羰基时,则R <2>为羧基或-CO 2 R <7>基(R <7>如上文所定义); 或(C)当R <1>是氢原子,Z是亚甲基,R然后<2>是羟甲基。 这样用于生产中间体的方法被描述。

    Method for producing 2-amino-6-halogenopurine and synthesis intermediate therefor
    90.
    发明公开
    Method for producing 2-amino-6-halogenopurine and synthesis intermediate therefor 失效
    Verfahren zur Herstellung von 2-Amino-6-Halogenopurin und Synthese einer Zwischenverbindung。

    公开(公告)号:EP0543095A2

    公开(公告)日:1993-05-26

    申请号:EP92114879.7

    申请日:1992-08-31

    IPC分类号: C07D473/40 C07D473/18

    CPC分类号: C07D473/40

    摘要: The present invention is directed to a method for producing a 2-amino-6-halogenopurine, a novel synthesis intermediate therefor and a method for producing said synthesis intermediate. The desired 2-amino-6-halogenopurine is an intermediate for the production of the compound useful as an antiviral agent, and by using the compound of the present invention as a starting material, the 2-amino-6-halogenopurine can be produced with high yield.

    摘要翻译: 本发明涉及一种2-氨基-6-卤代嘌呤的制备方法及其合成中间体及其制备方法。 所需的2-氨基-6-卤代嘌呤是用作生产用作抗病毒剂的化合物的中间体,通过使用本发明化合物作为起始原料,2-氨基-6-卤代嘌呤可以用 高产。