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    • 9. 发明申请
    • METHOD FOR PREPARING TRICYCLIC DERIVATIVES
    • 制备三环衍生物的方法
    • US20120101296A1
    • 2012-04-26
    • US13381036
    • 2010-06-29
    • Myung-Hwa KimIn-Hae YeJong-Hee Choi
    • Myung-Hwa KimIn-Hae YeJong-Hee Choi
    • C07C231/14C07C69/76C07C49/84C07C51/087
    • C07C319/20C07C51/06C07C65/01C07C67/08C07C67/30C07C233/65C07C235/42C07C2603/34C07D295/192C07C323/42C07C69/76
    • The present invention relates to a method for preparing a tricyclic derivative, and more particulary, to a method for preparing a tricyclic derivative inetermediate with high yield and purity, the method including: introducing a hydroxy group by esterifying and substituting 2-fluoroisophthalic acid compound; introducing a piperidyl group; introducing a hydroxy group through reduction reaction; and then hydrolyzing the resultant compound, and to a method for preparing the tricyclic derivative using said intermediate. According to the method of the present invention, it is possible to provide a tricyclic derivative and an intermediate thereof with high productivity and economic feasibility as well as high purity and yield, by purifying a compound using re-crystallization unlike typical methods of using column chromatography. In addition, the method of the present invention can be usefully used for industrial mass production because sodium borohydride or lithium aluminum hydride with low risk of a fire is used unlike typical methods of using lithium borohydride which is not industrially applicable due to high risk of a fire.
    • 本发明涉及一种制备三环衍生物的方法,更具体地说涉及一种以高产率和纯度制备三环衍生物三烯衍生物的方法,所述方法包括:通过酯化和取代2-氟间苯二甲酸化合物引入羟基; 引入哌啶基; 通过还原反应引入羟基; 然后水解所得化合物,以及使用所述中间体制备三环衍生物的方法。 根据本发明的方法,通过使用重结晶纯化化合物,可以提供具有高生产率和经济可行性以及高纯度和收率的三环衍生物及其中间体,与使用柱色谱法的典型方法不同 。 此外,本发明的方法可以有用地用于工业大规模生产,因为使用低风险的硼氢化钠或氢化铝锂不同于使用不具有工业上适用的硼氢化锂的典型方法,这是因为高风险的 火。