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    • 4. 发明申请
    • PROCESS FOR PREPARING 2-[(PYRIDINYL)METHYL]SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE
    • 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
    • WO2004111029A2
    • 2004-12-23
    • PCT/US2004/019001
    • 2004-06-10
    • TEVA PHARMACEUTICAL INDUSTRIES LTD.TEVA PHARMACEUTICALS USA, INC.LIEBERMAN, AnitaSINGER, ClaudeRAIZI, Yuriy
    • LIEBERMAN, AnitaSINGER, ClaudeRAIZI, Yuriy
    • C07D401/00
    • C07D401/12
    • 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.
    • 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。