wherein X is chloro or fluoro, by the strong acid solvolysis of an alpha-methylbenzylhydantoin of the formula:-;Also disclosed is a process for preparing compound (I) from a halochromanone oftheformula:-which processes proceeds through intermediate (V). Also covered are novel intermediates prepared in the above process, and the novel chiral hydantoin of the formula (I) in which X is chloro and a pharmaceutical composition containing it."/> Process for the preparation of chiral hydantoins, novel intermediates useful therein, and a novel hydantoin produced by said process and a pharmaceutical composition containing it
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Process for the preparation of chiral hydantoins, novel intermediates useful therein, and a novel hydantoin produced by said process and a pharmaceutical composition containing it

机译:制备手性乙内酰脲的方法,可用于其中的新型中间体以及通过所述方法生产的新型乙内酰脲和包含其的药物组合物

摘要

A process for preparing a chiral hydantoin aldose reductase inhibitor of the formula:wherein X is chloro or fluoro, by the strong acid solvolysis of an alpha-methylbenzylhydantoin of the formula:-;Also disclosed is a process for preparing compound (I) from a halochromanone oftheformula:-which processes proceeds through intermediate (V). Also covered are novel intermediates prepared in the above process, and the novel chiral hydantoin of the formula (I) in which X is chloro and a pharmaceutical composition containing it.
机译:制备下式的手性乙内酰脲醛糖还原酶抑制剂的方法: <图像文件=“ IMGA0001.GIF” he =“ 23” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 70” /> 其中X通过下式的α-甲基苄基乙内酰脲的强酸溶剂解是氯或氟 <图像文件=“ IMGA0002.GIF” he =“ 26” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 78” /> ;也公开了一种由式的卤代苯并二氢吡喃酮制备化合物(I)的方法: <图像文件=“ IMGA0003.GIF” he =“ 22” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 62” /> 处理继续通过中间体(V)。还涵盖了通过上述方法制备的新型中间体,以及其中X是氯的式(I)的新型手性乙内酰脲和包含它的药物组合物。

著录项

  • 公开/公告号EP0037672A3

    专利类型

  • 公开/公告日1983-08-24

    原文格式PDF

  • 申请/专利权人 PFIZER INC.;

    申请/专利号EP19810301247

  • 发明设计人 SARGES REINHARD;

    申请日1981-03-24

  • 分类号C07D491/107;C07D311/68;A61K31/415;C07D491/107;C07D311/00;C07D235/00;

  • 国家 EP

  • 入库时间 2022-08-22 10:33:57

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