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    • 5. 发明申请
    • Process for the purification of Montelukast
    • 蒙特鲁卡斯净化工艺
    • US20100029945A1
    • 2010-02-04
    • US12376773
    • 2007-08-07
    • Yolanda Gasanz GuillénPedro Talavera EscasanyMontserrat Monsalvatje Llagostera
    • Yolanda Gasanz GuillénPedro Talavera EscasanyMontserrat Monsalvatje Llagostera
    • C07D215/04
    • C07D215/18
    • It relates to a process for the purification of Montelukast, or pharmaceutically salts thereof, or solvates thereof, including stereoisomers or mixture thereof which comprises carrying out a specific set of selective solvent extractions of Montelukast or its impurities in a mixture of an organic solvent and water at specific ranges of pH and temperature which depend on the type of impurities to remove. In particular, it comprises at least one wash of an aqueous phase containing crude Montelukast in salt form with an organic solvent, at a pH comprised between 12.0 and 13.5; and optionally one or more washes of the resulting aqueous phase with an organic solvent at a pH comprised between 8.5 and 10.0. Montelukast is recovered by acidification at a pH comprised between 4.5 and 8.0 and solvent extraction, and is isolated either as acid or in salt form.
    • 本发明涉及纯化Montelukast或其药学上可接受的盐或其溶剂化物,包括立体异构体或其混合物的方法,其包括在有机溶剂和水的混合物中进行特定的选择性溶剂萃取孟鲁司特或其杂质 在特定的pH和温度范围内,这取决于要除去的杂质的类型。 特别地,其包含至少一次含有盐形式的粗壮孟鲁司特与有机溶剂的水相洗涤,pH在12.0和13.5之间; 并且任选地用pH为8.5至10.0的有机溶剂一次或多次洗涤所得水相。 通过在4.5至8.0之间的pH下酸化回收孟鲁司特并进行溶剂萃取,并以酸或盐形式分离。