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    • 2. 发明申请
    • METHOD FOR PREPARING TRICYCLIC DERIVATIVES
    • 制备三环衍生物的方法
    • WO2011004980A2
    • 2011-01-13
    • PCT/KR2010004212
    • 2010-06-29
    • JE IL PHARMACEUTICAL CO LTDKIM MYUNG-HWAYE IN-HAECHOI JONG-HEE
    • KIM MYUNG-HWAYE IN-HAECHOI JONG-HEE
    • C07C231/02C07C51/367C07C63/68C07C237/38
    • C07C319/20C07C51/06C07C65/01C07C67/08C07C67/30C07C233/65C07C235/42C07C2603/34C07D295/192C07C323/42C07C69/76
    • The present invention relates to a method for preparing tricyclic derivatives, and more particularly, to a method for preparing intermediates of novel tricyclic derivatives having a superior yield rate and purity, wherein the method involves esterifying 2-fluoroisophthalic acid compounds, conducting a substation reaction on the compounds to introduce a hydroxyl group, introducing a piperidyl group, conducting a reduction reaction on the compounds, introducing a hydroxyl group, and conducting a hydrolysis on the resultant compounds. The present invention also relates to a method for preparing tricyclic derivatives using the intermediates. The method of the present invention refines substances by recrystallization as opposed to conventional methods which involve refining substances by column chromatography, and thus prepares tricyclic derivatives having more excellent productivity, economical advantages, and higher purity and yield rate as compared to conventional methods, as well as to intermediates of the tricyclic derivatives. In addition, the method of the present invention uses sodium borohydride or lithium aluminum hydrate which have less risk of fire as opposed to conventional methods using lithium borohydrides which cannot be industrially used due to the high risk of fire thereof, and therefore the method of the present invention can be useful in industrial mass production.
    • 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制备具有优异的收率和纯度的新型三环衍生物的中间体的方法,其中该方法包括酯化2-氟间苯二甲酸化合物,进行变电站反应 引入羟基的化合物,引入哌啶基,对化合物进行还原反应,引入羟基,并在所得化合物上进行水解。 本发明还涉及使用中间体制备三环衍生物的方法。 本发明的方法与通过柱色谱法精炼物质的常规方法不同,通过重结晶来精制物质,因此制备与常规方法相比具有更优异的生产率,经济优点和更高的纯度和产率的三环衍生物,以及 关于三环衍生物的中间体。 此外,本发明的方法使用具有较低火焰危险性的硼氢化钠或氢氧化锂铝水合物,与常规方法相比,由于其具有高的火焰危险而不能在工业上使用的硼氢化锂,因此, 本发明可用于工业批量生产。