发明公开
EP0812827A1 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
- 专利标题: Piperidine derivative as intermediates for the preparation of paroxetine and process for their preparation
- 专利标题(中): 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
-
申请号: EP97303647.8申请日: 1997-05-29
-
公开(公告)号: EP0812827A1公开(公告)日: 1997-12-17
- 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.
- 申请人: SUMIKA FINE CHEMICALS Co., Ltd.
- 申请人地址: 3-1-21, Utajima, Nishiyodogawa-ku Osaka-shi, Osaka JP
- 专利权人: SUMIKA FINE CHEMICALS Co., Ltd.
- 当前专利权人: SUMIKA FINE CHEMICALS Co., Ltd.
- 当前专利权人地址: 3-1-21, Utajima, Nishiyodogawa-ku Osaka-shi, Osaka JP
- 代理机构: Marchant, James Ian
- 优先权: JP175893/96 19960613; JP294585/96 19961015; JP303838/96 19961029; JP326177/96 19961120; JP50980/97 19970218
- 主分类号: C07D211/22
- 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.
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.
公开/授权文献
信息查询