首页> 外国专利> A method of producing 5-amino-4-(1-cyclopropylnaphthalen-4-yl)-4H-1,2,4-triazole-3-thiol, a key intermediate for the production of 2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4H-1,2,4-triazol-3ylthio)acetic acid - lesinurade

A method of producing 5-amino-4-(1-cyclopropylnaphthalen-4-yl)-4H-1,2,4-triazole-3-thiol, a key intermediate for the production of 2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4H-1,2,4-triazol-3ylthio)acetic acid - lesinurade

机译:一种生产5-氨基-4-(1-环丙基萘-4-基)-4H-1,2,4-三唑-3-硫醇的方法,该中间体是生产2-(5-溴-4- (1-环丙基萘-4-基)-4H-1,2,4-三唑-3基硫基)乙酸-莱西努拉

摘要

the solution relates to the improved production method of highly pure intermediu00e1tu 5 - amino - 4 - (1 - cyklopropylnaftalen - 4 - yl) - 4h - 1,2,4-triazole - 3 - thiol moiety to form the formula.a key intermediate in the production of 2 - (5 - bromine - 4 - (1 - cyclopropyl - naphthalene - 4 - yl) - 4h - 1,2,4-triazole - 3 - ylthio) acetic acid formula ii, known under the generic name lesinurad.highly pure intermediu00e1t prepare response 4 - cyclopropyl - 1 - naftylisothiokyanu00e1tu with appropriate with - alkylthiosemikarbazidem in a suitable solvent.lesinurad is a selective inhibitor of the transport of uric acid lowering uric acid level in the blood.it is used in combination with any of the drugs acting as inhibitors of xanthin oxidase patients reach the satisfactory condition treatment using the xanthin oxidase inhibitors.
机译:该解决方案涉及改进的高纯度中间体5-氨基-4-(1-环丙基萘基-4-基)-4h-1,2,4-三唑-3-硫醇部分的制备方法。通式Ⅱ已知的生产2-(5-溴-4-(1-环丙基-萘-4-基)-4h-1,2,4-三唑-3-乙硫基)乙酸的主要中间体名称lesinurad。高纯度中间体制备反应4-环丙基-1-萘基异硫氰酸盐与适当的烷基硫半氨基苯乙酰胺在适当的溶剂中混合.lesinurad是选择性的尿酸转运抑制剂,可降低血液中的尿酸水平。与黄嘌呤氧化酶抑制剂的任何药物合用时,使用黄嘌呤氧化酶抑制剂可达到令人满意的治疗状态。

著录项

  • 公开/公告号CZ2016-491A3

    专利类型

  • 公开/公告日2018-02-21

    原文格式PDF

  • 申请/专利权人 ZENTIVA K.S.;

    申请/专利号CZ2016-491

  • 发明设计人 JAN STACH;STANISLAV RÁDL;ALEŠ HALAMA;

    申请日2016-08-11

  • 分类号C07D249/12;C07D249/14;

  • 国家 CZ

  • 入库时间 2022-08-21 12:53:06

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