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    METHOD FOR PREPARING TRICYCLIC DERIVATIVES
    2.
    发明公开
    METHOD FOR PREPARING TRICYCLIC DERIVATIVES 有权
    VERFAHREN ZUR HERSTELLUNG TRIZYKLISCHER DERIVATE

    公开(公告)号：EP2452931A4

    公开(公告)日：2013-12-25

    申请号：EP10797254

    申请日：2010-06-29

    申请人： JEIL PHARMACEUTICAL CO LTD

    发明人： KIM MYUNG-HWA ,  YE IN-HAE ,  CHOI JONG-HEE

    IPC分类号： C07C51/367 ,  C07C63/68 ,  C07C233/65 ,  C07C235/42 ,  C07C319/20 ,  C07C323/42 ,  C07D211/06

    CPC分类号： C07C319/20 ,  C07C51/06 ,  C07C65/01 ,  C07C67/08 ,  C07C67/30 ,  C07C233/65 ,  C07C235/42 ,  C07C2603/34 ,  C07D295/192 ,  C07C323/42 ,  C07C69/76

    摘要： 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.

    摘要翻译： 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批量生产，因为使用低的火焰危险的硼氢化钠或氢化铝锂不同于使用硼氢化锂的典型方法，因为硼氢化锂不是工业上适用的，因为高风险 火。

    NOVEL {4-[2-(DIMETHYLAMINO)-1-(1-HYDROXYCYCLOHEXYL)ETHYL]PHENOXY}PHOSPHATE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, A PRODUCTION METHOD THEREFOR AND A PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS CONTAINING THE SAME AS AN ACTIVE COMPONENT
    10.
    发明公开
    NOVEL {4-[2-(DIMETHYLAMINO)-1-(1-HYDROXYCYCLOHEXYL)ETHYL]PHENOXY}PHOSPHATE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, A PRODUCTION METHOD THEREFOR AND A PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS CONTAINING THE SAME AS AN ACTIVE COMPONENT 审中-公开
    NEW {4- [2-（二甲基氨基）-1-（1-羟基环己基）乙基]苯氧基}磷酸酯或其药学上可接受的盐，其制备方法和药物组合物含作为用于CNS病症的预防和治疗的有效成分

    公开(公告)号：EP2287171A2

    公开(公告)日：2011-02-23

    申请号：EP09742862.7

    申请日：2009-05-08

    申请人： Jeil Pharmaceutical Co., Ltd.

    发明人： KANG, Seok Won ,  CHUN, Jong Soo ,  KANG, Heung Mo ,  HONG, Eui Seok ,  CHUN, Kwang-Woo ,  BYUN, Young Seok ,  KIM, Myung-Hwa ,  MOON, Young Il ,  RYU, Jei Man

    IPC分类号： C07F9/22

    CPC分类号： C07F9/12

    摘要： The present invention relates to a novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof, a production method therefor and a pharmaceutical composition for preventing and treating central nervous system disorders which contains the same as an active component. The novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof according to the present invention can beneficially be used to prevent and treat central nervous system disorders since it exhibits an equivalent biological and pharmacological activity to venlafaxine and salts thereof which are known in the field, it has very little toxicity, and, in particular, it is outstandingly soluble in water as compared with prior-art venlafaxine derivatives.

    摘要翻译： 本发明涉及一种新型的{4- [2-（二甲基氨基）-1-（1-羟基环己基）乙基]苯氧基}磷酸酯或其药学上可接受的盐，其制造方法及用于预防和治疗中枢神经的药物组合物 系统紊乱其中包含了相同活性组分。 该新型{4- [2-（二甲基氨基）-1-（1-羟基环己基）乙基]苯氧基}磷酸酯或其药学上可接受的盐gemäß到本发明可有利地用于预防和，因为它展品治疗中枢神经系统疾病 在同等的生物活性和药理活性，以文拉法辛及其盐其中在字段是已知的，它具有非常小的毒性，而且，特别地，它是作为与现有技术的文拉法辛衍生物相比显着地溶于水。