发明授权
US07973182B2 Process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols
有权
用于制备对映体纯的1-取代-3-氨基醇的方法
- 专利标题: Process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols
- 专利标题(中): 用于制备对映体纯的1-取代-3-氨基醇的方法
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申请号: US10590140申请日: 2005-02-21
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公开(公告)号: US07973182B2公开(公告)日: 2011-07-05
- 发明人: Dominique Michel , Hanspeter Mettler , John McGarrity
- 申请人: Dominique Michel , Hanspeter Mettler , John McGarrity
- 申请人地址: CH Basel
- 专利权人: Lonza Ltd.
- 当前专利权人: Lonza Ltd.
- 当前专利权人地址: CH Basel
- 代理机构: Fisher, Christen & Sabol
- 优先权: EP04003809 20040219; EP04010043 20040428
- 国际申请: PCT/EP2005/001781 WO 20050221
- 国际公布: WO2005/080370 WO 20050901
- 主分类号: C07D307/02
- IPC分类号: C07D307/02 ; C07D333/20
摘要:
A process for the preparation of enantiomerically pure 1-substituted-3-amino-alcohols, particularly of (S)-(−)- and (R)-(+)-3-N-methylamino-1-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of the formula: wherein R1 is 2-thienyl, 2-furanyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein R2 is C1-4-alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups. The corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Salts of a carboxylic acid with the aminoketones and the aminoalcohols obtained by asymmetrically hydrogenating the aminoketones, respectively.
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