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    Method for producing dibenzothiepin derivative
    4.
    发明专利
    Method for producing dibenzothiepin derivative 审中-公开
    生产二苯唑来汀衍生物的方法

    公开(公告)号：JP2005139120A

    公开(公告)日：2005-06-02

    申请号：JP2003377810

    申请日：2003-11-07

    申请人： Ohara Yakuhin Kogyo Kk ,  大原薬品工業株式会社

    发明人： NAKADA YOSHITAKA

    IPC分类号： C07D337/14 ,  C07B61/00 ,  C07C319/20 ,  C07C323/63

    摘要： PROBLEM TO BE SOLVED: To provide a method for industrially advantageously producing zaltoprofen as an anti-inflammatory/analgesic agent.
    SOLUTION: The method comprises the following process: Zinc iodide, sodium cyanide or potassium cyanide, and trimethylsilyl chloride are added to a compound of formula(I) followed by mixing them together to carry out a reaction to form a compound of formula(II). Sodium cyanide or potassium cyanide, trimethylsilyl chloride, acetonitrile and water are added to the compound of formula(II) followed by mixing them together to carry out a reaction to form a compound of formula(III). Polyphosphoric acid is made to act on the compound of formula(III) to effect cyclization, followed by addition of water to form a compound of formula(IV), which is then hydrolyzed to obtain the objective compound(zaltoprofen) of formula(V). In the above formulas, R is a lower alkyl.
    COPYRIGHT: (C)2005,JPO&NCIPI

    摘要翻译： 待解决的问题：提供一种在工业上有利地制备作为抗炎/止痛剂的扎洛芬的方法。 解决方案：该方法包括以下过程：将碘化锌，氰化钠或氰化钾和三甲基甲硅烷基氯加入到式（I）化合物中，然后将它们混合在一起进行反应，形成式 （II）。 将氰化钠或氰化钾，三甲基甲硅烷基氯，乙腈和水加入到式（II）化合物中，然后将它们混合在一起进行反应以形成式（III）化合物。 使多磷酸作用于式（III）化合物进行环化，然后加入水形成式（IV）化合物，然后将其水解，得到式（V）的目标化合物（zaltoprofen） 。 在上式中，R为低级烷基。 版权所有（C）2005，JPO＆NCIPI

    TREATING AGENT OF HYPERURICEMIA
    8.
    发明专利
    TREATING AGENT OF HYPERURICEMIA 失效

    公开(公告)号：JPH0341022A

    公开(公告)日：1991-02-21

    申请号：JP17682589

    申请日：1989-07-07

    申请人： HOE YAKUKOU KK ,  PROD DEV RES INST

    发明人： KAIO SUMINORI ,  YABUUCHI TAKAHIRO ,  UMEKAWA TOMOMICHI

    IPC分类号： C07D337/14 ,  A61K31/35 ,  A61K31/38 ,  A61P19/06 ,  C07D313/14

    摘要： PURPOSE:To obtain a treating agent of hyperuricemia having low side effects specific to psychotropic agents, such as suppressive action on nervous system, comprising a dibenzothiepin (or debenzoxepin) derivative, which is novel except a part of the derivatives. CONSTITUTION:A treating agent of hyperuricemia which comprises a compound shown by formula I (Y is S or O; X is H, halogen or lower alkoxy; R is 3-4C alkylene; R and R are methyl or ethyl), such as 8-chloro-10-(3- dimethylaminopropoxy)dibenzo [b,f]thiepin or dibenzoxepin or a pharmaceutically acceptable salt as an active ingredient and can promote discharge of uric acid and urination without causing side effects such as dizziness, unsteadiness, sleepfulness, headache, weakness and malaise owing to the absence of suppressive action on nervous system frequently observed in similar well-known drug. The above-mentioned compound is obtained by reacting a compound shown by formula II with an alcohol reactive derivative shown by formula III.