发明授权
US07186865B2 Optically active 1-(fluoro-, trifluoromethyl-or trifluoromethoxy-substituted phenyl) alkylamine n-monoalkyl derivatives and process for producing same
有权
光学活性1-(氟 - ,三氟甲基 - 或三氟甲氧基取代的苯基)烷基胺n-单烷基衍生物及其制备方法
- 专利标题: Optically active 1-(fluoro-, trifluoromethyl-or trifluoromethoxy-substituted phenyl) alkylamine n-monoalkyl derivatives and process for producing same
- 专利标题(中): 光学活性1-(氟 - ,三氟甲基 - 或三氟甲氧基取代的苯基)烷基胺n-单烷基衍生物及其制备方法
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申请号: US10476650申请日: 2003-09-05
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公开(公告)号: US07186865B2公开(公告)日: 2007-03-06
- 发明人: Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
- 申请人: Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
- 申请人地址: JP Ube
- 专利权人: Central Glass Company, Limited
- 当前专利权人: Central Glass Company, Limited
- 当前专利权人地址: JP Ube
- 代理机构: Crowell & Moring LLP
- 优先权: JP2002-261148 20020906
- 国际申请: PCT/JP03/11341 WO 20030905
- 国际公布: WO2004/022521 WO 20040318
- 主分类号: C07C211/00
- IPC分类号: C07C211/00
摘要:
An optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula 4 is produced by a process including (a) reacting an optically active secondary amine, represented by the formula 1, with an alkylation agent R2—X, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula 3; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative, wherein R represents a fluorine atom, trifluoromethyl group or trifluoromethoxy group, n represents an integer of from 1 to 5, each of R1 and R2 independently represents an alkyl group having a carbon atom number of from 1 to 6, Me represents a methyl group, Ar represents a phenyl group or 1- or 2-naphthyl group, * represents a chiral carbon, and X represents a leaving group.