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    PROCESSES FOR PREPARING ARMODAFINIL INTERMEDIATE
    2.
    发明申请
    PROCESSES FOR PREPARING ARMODAFINIL INTERMEDIATE 审中-公开
    制备ARMODAFINIL中间体的方法

    公开(公告)号：WO2008070143A1

    公开(公告)日：2008-06-12

    申请号：PCT/US2007/024972

    申请日：2007-12-05

    Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD. ,  TEVA PHARMACEUTICALS USA, INC. ,  DOLITZKY, Ben-zion ,  CHEN, Kobi

    Inventor： DOLITZKY, Ben-zion ,  CHEN, Kobi

    IPC: C07B55/00 ,  C07C315/04 ,  C07C317/44

    CPC classification number: C07C315/04 ,  C07B55/00 ,  C07C317/44

    Abstract: The present invention encompasses processes (1) for preparing racemic 2-(benzhydrylsulfinyl)acetic acid by combining the (S)- or the (R)-enantiomer with at least one organic solvent and at least one acid promoter, such as perchloric acid or an acyl halide; (2) for preparing racemic 2-(benzhydrylsulfinyl)acetamide or racemic 2-(benzhydrylsulfinyl)acetic acid by combining the (S)- or the (R)-enantiomer with at least one organic solvent having a boiling point above 60°C, heating to a temperature above 60°C and cooling. The present invention also encompasses the conversion of the racemic intermediates to armodfinil.

    Abstract translation: 本发明包括通过将（S） - 或（R） - 对映异构体与至少一种有机溶剂和至少一种酸促进剂如高氯酸或高氯酸反应制备外消旋2-（二苯甲基亚磺酰基）乙酸的方法（1） 酰卤; （2）通过将（S） - 或（R） - 对映体与至少一种沸点高于60℃的有机溶剂组合来制备外消旋2-（二苯甲基亚磺酰基）乙酰胺或外消旋2-（二苯甲基亚磺酰基）乙酸， 加热到60℃以上的温度并冷却。 本发明还包括将外消旋中间体转化成犰狳。

    PROCESS FOR PREPARING 2-[(PYRIDINYL)METHYL]SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE
    6.
    发明申请
    PROCESS FOR PREPARING 2-[(PYRIDINYL)METHYL]SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE 审中-公开
    制备2- [（吡啶基）甲基]磺酰基取代苯并咪唑和新戊酰氯的衍生物的方法

    公开(公告)号：WO2004111029A3

    公开(公告)日：2005-11-17

    申请号：PCT/US2004019001

    申请日：2004-06-10

    Applicant: TEVA PHARMA ,  TEVA PHARMA ,  LIBERMAN ANITA ,  SINGER CLAUDE ,  RAIZI YURIY ,  BRAUDE VIVIANA ,  FINKELSTEIN NINA ,  CHEN KOBI ,  PILARSKY GIDEON

    Inventor： LIBERMAN ANITA ,  SINGER CLAUDE ,  RAIZI YURIY ,  BRAUDE VIVIANA ,  FINKELSTEIN NINA ,  CHEN KOBI ,  PILARSKY GIDEON

    IPC: C07D401/12 ,  A61K31/44 ,  A61P1/04

    CPC classification number: C07D401/12

    Abstract: 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.

    Abstract translation: 本发明提供了一种方法，其包括将硫醚与约1.05至约1.6摩尔当量的活性氯氧化剂，优选次氯酸钠和约2.5至约5.0摩尔当量碱金属碱混合; 并回收优选泮托拉唑，兰索拉唑，奥美拉唑或雷贝拉唑的亚砜。 该方法可以进一步包括使亚砜与钠离子源（优选氢氧化钠）接触以产生亚砜的钠盐。 本发明还涉及泮托拉唑的新型氯化衍生物，其包括5（二氟甲氧基）-2 - [[（3,4-二甲氧基-2-吡啶基） - 氯甲基]亚磺酰基] -1H-苯并咪唑和5-（二氟甲氧基）-2- [ [（3,4-二甲氧基-2-吡啶基）氯羟甲基]亚磺酰基] -1H-苯并咪唑及其制备方法。 本发明还涉及在泮托拉唑和至少一种其它化合物的混合物中量化和鉴定泮托拉唑以外的化合物的方法。

    PROCESS FOR PREPARING 2-[(PYRIDINYL)METHYL]SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE
    7.
    发明申请
    PROCESS FOR PREPARING 2-[(PYRIDINYL)METHYL]SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE 审中-公开
    制备2 - [（吡啶基）甲基]亚磺酰基 - 取代的苯并咪唑和新型氯化吡唑衍生物的方法

    公开(公告)号：WO2004111029A8

    公开(公告)日：2005-04-21

    申请号：PCT/US2004019001

    申请日：2004-06-10

    Applicant: TEVA PHARMA ,  TEVA PHARMA ,  LIBERMAN ANITA ,  SINGER CLAUDE ,  RAIZI YURIY ,  BRAUDE VIVIANA ,  FINKELSTEIN NINA ,  CHEN KOBI ,  PILARSKY GIDEON

    Inventor： LIBERMAN ANITA ,  SINGER CLAUDE ,  RAIZI YURIY ,  BRAUDE VIVIANA ,  FINKELSTEIN NINA ,  CHEN KOBI ,  PILARSKY GIDEON

    IPC: C07D401/12 ,  C07D401/00

    CPC classification number: C07D401/12

    Abstract: 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.

    Abstract translation: 本发明提供了一种方法，该方法包括将硫醚与约1.05至约1.6摩尔当量的活性含氯氧化剂，优选次氯酸钠和约2.5至约5.0摩尔当量的碱金属碱混合; 并回收优选泮托拉唑，兰索拉唑，奥美拉唑或雷贝拉唑的亚砜。 该方法还可以包括使亚砜与钠离子源，优选氢氧化钠接触以产生亚砜的钠盐。 本发明还涉及泮托拉唑的新型氯化衍生物，包括5-（二氟甲氧基）-2 - [[（3,4-二甲氧基-2-吡啶基） - 氯甲基]亚磺酰基] -1H-苯并咪唑和5-（二氟甲氧基） [（3,4-二甲氧基-2-吡啶基）氯羟甲基]亚磺酰基] -1H-苯并咪唑及其制备方法。 本发明还涉及在泮托拉唑与至少一种其他化合物的混合物中定量和鉴定不同于泮托拉唑的化合物的方法。

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