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

申请人： SUMIKA FINE CHEMICALS Co., Ltd.

发明人： Sugi, Kiyoshi, c/o Sumika Fine Chem. Co., Ltd. ,  Itaya, Nobushige, c/o Sumika Fine Chem. Co., Ltd. ,  Katsura, Tadashi, c/o Sumika Fine Chem. Co., Ltd. ,  Igi, Masami, c/o Sumika Fine Chem. Co., Ltd. ,  Yamazaki, Shigeya, c/o Sumika Fine Chem. Co., Ltd. ,  Ishibashi, Taro, c/o Sumika Fine Chem. Co., Ltd. ,  Yamaoka, Teiji, c/o Sumika Fine Chem. Co., Ltd. ,  Kawada, Yoshihiro, c/o Sumika Fine Chem. Co., Ltd. ,  Tagami, Yayoi, c/o Sumika Fine Chem. Co., Ltd.

IPC分类号： C07D211/22

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 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。