IMPROVED PROCESS FOR THE SYNTHESIS OF ENANTIOMERIC INDANYLAMINE DERIVATIVES
    6.
    发明公开
    IMPROVED PROCESS FOR THE SYNTHESIS OF ENANTIOMERIC INDANYLAMINE DERIVATIVES 审中-公开
    VERBESSERTES VERFAHREN ZUR SYNTHESE ENANTIMERISCHER INDANYLAMIN-DERIVATE

    公开(公告)号:EP1851188A1

    公开(公告)日:2007-11-07

    申请号:EP06765604.1

    申请日:2006-02-20

    摘要: A process for manufacturing (R)-propynylaminoindans, and alternatively, a process for manufacturing (S)- propynylaminoindans. The chiral propynylaminoindans include alkoxy or alkylcarbamates derivatives. The process comprises transfer or pressure hydrogenation in the presence of an optically active catalyst to reduce 1-indanones. The chiral product, either (S)- or (R)- indanols undergo nucleophilic substitution to produce the named product. In an additional aspect, the invention relates to novel intermediates and compounds, namely, substituted indanones, substituted (S)- indanols and substituted (R)- indanols.

    摘要翻译: 制备(R) - 丙炔基氨基茚满的方法,或者,制备(S) - 丙炔基氨基茚满的方法。 手性丙炔基氨基甘氨酸包括烷氧基或烷基氨基甲酸酯衍生物。 该方法包括在光学活性催化剂的存在下转移或加压氢化以还原1-茚满酮。 (S) - 或(R) - 茚满醇的手性产物经历亲核取代产生命名的产物。 在另一方面,本发明涉及新的中间体和化合物,即取代的茚满酮,取代的(S) - 茚满醇和取代的(R) - 茚满醇。

    PROCESS FOR PREPARING 2-(PYRIDINYL)METHYL SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE
    9.
    发明公开
    PROCESS FOR PREPARING 2-(PYRIDINYL)METHYL SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE 审中-公开
    用于生产(吡啶基)甲基亚磺酰基的苯并咪唑取代的和泮托拉唑的新氯化衍生物

    公开(公告)号:EP1615913A2

    公开(公告)日:2006-01-18

    申请号:EP04755278.1

    申请日:2004-06-10

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12

    摘要: The present invention provides a process comprising admixing a thioether with about 1.05 to about 1.6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorite, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide that is preferably pantoprazole, lansoprazole, omeprazole, or rabeprazole. The process may further comprise contacting the sulfoxide with a source of sodium ions, preferably sodium hydroxide, to produce the sodium salt of the sulfoxide. The invention also relates to novel chlorinated derivatives of pantoprazole including 5­(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H- benzimidazole and 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)­chlorohydroxymethyl] sulfinyl]-1H-benzimidazole and processes for making them. The invention also relates to processes of quantifying and identifying a compound other than pantoprazole in a mixture of pantoprazole and at least one other compound.