무수 아리피프라졸 결정의 제조방법
    2.
    发明授权
    무수 아리피프라졸 결정의 제조방법 有权
    制备无水阿立哌唑晶体的方法

    公开(公告)号:KR101372840B1

    公开(公告)日:2014-03-12

    申请号:KR1020120084839

    申请日:2012-08-02

    CPC classification number: C07D311/20

    Abstract: 본 발명은 신규의 무수 아리피프라졸 결정, 즉 7.6, 8.0, 13.4, 13.8, 20.4, 22.1, 22.5, 및 24.1 °2θ(± 0.2°)에서 피크를 갖는 분말 X-선 회절 스펙트럼을 갖는 무수 아리피프라졸 결정의 제조방법을 제공한다. 본 발명의 제조방법에 따라 얻어진 무수 아리피프라졸 결정은 가속조건하에서도 고유의 융점(148 ∼ 149 ℃의 융점)을 그대로 유지함으로써 결정형의 변화를 나타내지 않는다. 또한, 흡습성이 매우 낮고, 광안정성이 우수함으로써 효율적인 제제화가 가능하다.

    무수 아리피프라졸 결정의 제조방법
    7.
    发明公开
    무수 아리피프라졸 결정의 제조방법 有权
    制备无水阿维拉唑晶体的方法

    公开(公告)号:KR1020140018567A

    公开(公告)日:2014-02-13

    申请号:KR1020120084839

    申请日:2012-08-02

    CPC classification number: C07D311/20

    Abstract: The present invention provides a preparing method of novel anhydrous aripiprazole crystals which has a powder X-ray diffraction spectrum having peaks at 7.6, 8.0, 13.4, 13.8, 20.4, 22.1, 22.5, and 24.1°2θ(± 0.2°). The anhydrous aripiprazole crystals obtained according to the method of the present invention do not exhibit changes in crystal form by maintaining an inherent melting point (meting point of 148-149°C) which is unchanged even under accelerated conditions. Also, the present invention can be made into an efficient preparation since the hygroscopic properties are very low and the light stability is outstanding.

    Abstract translation: 本发明提供一种新型无水阿立哌唑晶体的制备方法,其具有在7.6,8.0,13.4,13.8,20.4,22.1,22.5和24.1°2θ(±0.2°)具有峰的粉末X射线衍射光谱。 根据本发明的方法获得的无水阿立哌唑晶体通过保持甚至在加速条件下不变的固有熔点(温度为148-149℃)也不会发生晶体形态变化。 此外,由于吸湿性能非常低并且光稳定性突出,本发明可以制成有效的制备方法。

    벤조피란-2-올 유도체의 생성 방법
    8.
    发明公开
    벤조피란-2-올 유도체의 생성 방법 失效
    生产苯二甲醛衍生物的方法

    公开(公告)号:KR1020090003353A

    公开(公告)日:2009-01-09

    申请号:KR1020087028577

    申请日:2007-05-21

    Abstract: The invention provides a process for the production of a compound of formula (I), wherein Y is selected from CH3, CH2OH, CH2CH2OH, CH2Br and Br; comprising the steps of: (i) reacting a compound of formula (II), wherein OX is hydroxy or O- M+, in which M+ is a cation selected from Li+, Na+ and K+, and Y is as defined above; with trans-cinnamaldehyde (III), in the presence of a secondary amine compound; then (ii) treating the product of the preceding step with acid to afford the compound of formula (I). The above process may be used in the production of tolterodine and fesoterodine, which are useful in the treatment of overactive bladder.

    Abstract translation: 本发明提供了制备式(I)化合物的方法,其中Y选自CH 3,CH 2 OH,CH 2 CH 2 OH,CH 2 Br和Br; 包括以下步骤:(i)使其中OX是羟基或O-M +的式(II)化合物与M +是选自Li +,Na +和K +的阳离子,Y如上定义; 在仲胺化合物的存在下反式肉桂醛(III); 然后(ii)用酸处理前述步骤的产物,得到式(I)化合物。 上述方法可用于生产托特罗定和非索罗定,其可用于治疗膀胱过度活动症。

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