发明公开
EP2365965A1 Process for manufacturing substituted 3-pyridylmethyl ammonium bromides
审中-公开
制备取代的3-吡啶基甲基溴化铵的方法
- 专利标题: Process for manufacturing substituted 3-pyridylmethyl ammonium bromides
- 专利标题(中): 制备取代的3-吡啶基甲基溴化铵的方法
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申请号: EP09755886.0申请日: 2009-11-13
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公开(公告)号: EP2365965A1公开(公告)日: 2011-09-21
- 发明人: GEBHARDT, Joachim , MENGES, Frederik , RACK, Michael , KEIL, Michael , SCHRÖDER, Jochen , ORSTEN, Stefan , ZECH, Helmut , KLIMA, Rodney, F. , CORTES, David , LEICHT, Robert , YEGERLEHNER, Tony
- 申请人: BASF SE
- 申请人地址: 67056 Ludwigshafen DE
- 专利权人: BASF SE
- 当前专利权人: BASF SE
- 当前专利权人地址: 67056 Ludwigshafen DE
- 代理机构: Rippel, Hans Christoph
- 优先权: US114230P 20081113
- 国际公布: WO2010055139 20100520
- 主分类号: C07D213/80
- IPC分类号: C07D213/80 ; C07D401/04 ; A61K31/44 ; A61K31/4439
摘要:
A process for manufacturing 5,6-disubstituted-3-pyridylmethyl ammonium bromides (I), wherein Q is a tertiary aliphatic or cyclic, saturated, partially unsaturated or aromatic amine; Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; Y and Y1 are each independently OR1, NR1R2, or when taken together YY1 is —O—, —S— or NR3—; R1 and R2 are each independently hydrogen, C1-C4 alkyl optionally substituted with C1-C4 alkoxy or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms, or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms; R3 is hydrogen or C1-C4 alkyl; comprises the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with bromine in the presence of a radical initiator in a solvent mixture comprising an aqueous phase and an organic phase, where the organic phase comprises a solvent selected from 1,2-dichloroethane, chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene and tetrachloromethane, and where the pH-value of the aqueous phase is from 3 to
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