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    • 5. 发明授权
    • 피타바스타틴 또는 그의 염의 중간체의 제조방법
    • 制备PITAVASTATIN或其盐的中间体的方法
    • KR100995882B1
    • 2010-11-22
    • KR1020100053631
    • 2010-06-08
    • 에이치 엘 지노믹스(주)
    • 이서진김현규
    • C07D215/04A61K31/43A61P3/06
    • C07D405/06A61K31/47C07D215/04C07D215/14
    • PURPOSE: A method for preparing pitavastatin or salt thereof is provided to avoid difficulty of handling intermediate compound of oil phase and to obtain a compound having dihydroxy moiety of high purity. CONSTITUTION: A method for preparing a compound of chemical formula 4 of solid crystal comprises: a step of reacting a compound of chemical formula 3 with a compound of chemical formula 2 under the presence of base; a step of adjusting the mixture at 40-45 °C; a step of adding alcohol of C1-C4 and cooling at 5-15 °C and precipitating; a step of washing precipitate with water and drying. A method for manufacturing pitavastatin or pharmaceutically acceptable salt thereof comprises: a step of preparing the compound of chemical formula 4; a step of adding acid to the compound of chemical formula 4; a step of converting to the compound of chemical formula 5; a step of NaOH to the compound of chemical formula 5; and a step of selectively converting pitavastatin free base to pharmaceutically acceptable salt.
    • 目的:提供一种制备匹伐他汀或其盐的方法,以避免难以处理油相的中间体化合物,并获得具有高纯度的二羟基部分的化合物。 构成:制备固体晶体化学式4的化合物的方法包括:使化学式3化合物与化学式2的化合物在碱存在下反应的步骤; 在40-45℃下调节混合物的步骤; 加入C1-C4醇并在5-15℃冷却并沉淀的步骤; 用水洗涤沉淀物并干燥的步骤。 制备匹伐他汀或其药学上可接受的盐的方法包括:制备化学式4的化合物的步骤; 向化学式4的化合物中加入酸的步骤; 转化为化学式5的化合物的步骤; NaOH化学式5化合物的步骤; 以及将匹伐他汀游离碱选择性地转化为药学上可接受的盐的步骤。