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    • 3. 发明申请
    • IMPROVED PREPARING METHOD OF (S)-OMEPRAZOLE FROM OMEPRAZOLE RACEMATE USING OPTICAL RESOLUTION AGENT
    • 使用光学分解剂改进从奥美拉唑的(S) - 甲基吡咯的制备方法
    • WO2009145368A1
    • 2009-12-03
    • PCT/KR2008/002961
    • 2008-05-27
    • SK CHEMICALS CO., LTD.KIM, Jae-SunLEE, Jin YoungKIM, Sun HoKIM, Nam hoLEE, Nam KyuPARK, Eun JuKUM, Do Seung
    • KIM, Jae-SunLEE, Jin YoungKIM, Sun HoKIM, Nam hoLEE, Nam KyuPARK, Eun JuKUM, Do Seung
    • C07D401/12C07D277/30A61K31/415A61K31/44
    • C07D401/12
    • The present invention relates to an improved preparing method of ( S )-omeprazole from omeprazole racemate. In an exemplary embodiment, the preparing method according to the present invention comprises the steps of: a) reacting omeprazole racemate with optically active diethyl-D-tartrate and a titanium compound in an alcohol solvent to prepare an omeprazole racemic complex; b) reacting the omeprazole racemic complex with 1.5-3.0 molar equivalents of ( S )-(+)-mandelic acid as optical resolution agent to prepare an optically active ( S )-omeprazole complex; and c) dissociating the optically active ( S) -omeprazole complex with a basic solution to prepare an ( S )-omeprazole free base or reacting the ( S )- omeprazole free base with a metal salt to transfer to a metal salt or a metal salt hydrate of ( S )- omeprazole. With optical purity of 99.0 %ee or better, the ( S )-omeprazole, the metal salt thereof or the hydrate thereof prepared in accordance with the present invention is useful as a medicinal material.
    • 本发明涉及一种改善奥美拉唑外消旋物(S) - 奥美拉唑的制备方法。 在一个示例性实施方案中,根据本发明的制备方法包括以下步骤:a)使奥美拉唑外消旋物与光学活性的D-酒石酸二乙酯和钛化合物在醇溶剂中反应以制备奥美拉唑外消旋体; b)将奥美拉唑外消旋配合物与1.5-3.0摩尔当量的(S) - (+) - 扁桃酸作为光学拆分剂反应,制备光学活性(S) - 奥美拉唑复合物; 和c)用碱性溶液解离光学活性(S) - 奥美拉唑复合物以制备(S) - 奥美拉唑游离碱或使(S) - 奥美拉唑游离碱与金属盐反应转移至金属盐或金属 (S) - 奥美拉唑盐水合物。 光学纯度为99.0%ee或更好,根据本发明制备的(S) - 奥美拉唑,其金属盐或其水合物可用作药用材料。