利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

3 条记录 (耗时 0.008 秒)

    Process for preparing leflunomide form I
    1.
    发明授权
    Process for preparing leflunomide form I 失效
    制备来氟米特I的方法

    公开(公告)号：US06806373B2

    公开(公告)日：2004-10-19

    申请号：US10410493

    申请日：2003-04-08

    申请人： Iiya Avrutov ,  Neomi Gershon ,  Judith Aronhime

    发明人： Iiya Avrutov ,  Neomi Gershon ,  Judith Aronhime

    IPC分类号： C07B2600

    CPC分类号： C07D261/18 ,  A61K31/42

    摘要： New leflunomide Form III is disclosed, along with processes for preparing it. The present invention also provides an economic process for preparing leflunomide Form II and a process for preparing leflunomide Form I from leflunomide Form III. Pharmaceutical compositions and dosage forms containing the new form and methods of using them for the treatment of rheumatoid arthritis are also disclosed.

    摘要翻译： 公开了新的来氟米特III型，以及其制备方法。 本发明还提供了用于制备来氟米特II型的经济方法和从来氟米特III型制备来氟米特I型的方法。 还公开了含有将其用于治疗类风湿性关节炎的新形式和方法的药物组合物和剂型。

    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same
    3.
    发明授权
    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same 失效
    用于制备克拉霉素和克拉霉素中间体，基本上不含肟的克拉霉素的方法和包含其的药物组合物

    公开(公告)号：US06617436B2

    公开(公告)日：2003-09-09

    申请号：US09736447

    申请日：2000-12-15

    申请人： Iiya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    发明人： Iiya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    IPC分类号： C07H100

    CPC分类号： C07H17/08 ,  C07F7/1892

    摘要： The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′, 4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with methylating agent in the presence of at least one solvent and a base, where the solvent comprises methyl tertbutyl ether. Processes for converting protected silylated clarithromycin oxime to clarithromycin according to the present invention, include reacting protected silylated clarithromycin oxime with ethanol and water at an ethanol to water ratio of about 1:1, in the presence of an acid and a deoximating agent and cooling the reaction mixture prior to adding sodium hydroxide, where the process takes place without any additional water addition. Further processes for converting protected silylated clarithromycin oxime to clarithromycin, include heating a mixture of protected silylated clarithromycin oxime, acid, and deoximating agent in an ethanol/water solvent to reflux for more than 4 hours, with a two-fold addition of deoximating agent to produce essentially oxime-free clarithromycin.

    摘要翻译： 本发明涉及制备受保护的甲硅烷基化克拉霉素肟，优选6-O-甲基-2'，4“ - 双（三甲基甲硅烷基） - 红霉素A 9-O-（2-甲氧基丙-2-基）肟（” S-MOP肟“），并将保护的甲硅烷基化克拉霉素肟（优选S-MOP肟）转化为克拉霉素。 根据本发明的制备受保护的甲硅烷基化克拉霉素肟的方法包括使甲硅烷基肟衍生物与甲基化剂在至少一种溶剂和碱的存在下反应，其中溶剂包括甲基叔丁基醚。 将受保护的甲硅烷基化克拉霉素肟转化为克拉霉素的方法包括在酸和脱肟剂的存在下，将保护的甲硅烷基化克拉霉素肟与乙醇和水以约1:1的乙醇与水反应并冷却 在加入氢氧化钠之前的反应混合物，其中该方法进行而没有任何额外的水添加。 将受保护的甲硅烷基化克拉霉素肟转化为克拉霉素的其它方法包括在乙醇/水溶剂中将受保护的甲硅烷基化克拉霉素肟，酸和脱肟剂的混合物加热回流4小时以上，加入二肟剂至 产生基本上无肟的克拉霉素。