首页> 外国专利> PROCESSES FOR PREPARING A FLUOROQUINOLONE AND PREPARING A CARBOXYLIC FLUORQUINOLONE ACID, ENANTIOMER OF A FLUOROQUINOLONE, A METHOD FOR CARRYING OUT AN ANTIMICROBIAN ACTIVITY, AND COMPOSITION.

PROCESSES FOR PREPARING A FLUOROQUINOLONE AND PREPARING A CARBOXYLIC FLUORQUINOLONE ACID, ENANTIOMER OF A FLUOROQUINOLONE, A METHOD FOR CARRYING OUT AN ANTIMICROBIAN ACTIVITY, AND COMPOSITION.

机译:制备氟喹诺酮和制备羧酸氟喹诺酮酸的方法,氟喹诺酮的对映体,进行抗微生物活性的方法和组成。

摘要

A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
机译:如本文所示,制备具有式I,Ia或IV的喹诺酮羧酸或其衍生物的方法包括使用在喹诺酮环上一个或多个特定位置已经具有一个或多个所需取代基的起始喹诺酮,并保留该喹诺酮羧酸。在整个合成过程中这些取代基的取向。与现有技术的方法相比,本发明的方法包括更少的步骤。本方法还可以包括从对映体混合物中简单地分离出所需的喹诺酮羧酸或其衍生物的对映体。通过本发明方法制备的包含氟喹诺酮类的药物组合物可以有效地用于抵抗多种微生物病原体。

著录项

  • 公开/公告号BRPI0806581A2

    专利类型

  • 公开/公告日2014-05-06

    原文格式PDF

  • 申请/专利权人 BAUSCH & LOMB INCORPORATED;

    申请/专利号BR2008PI06581

  • 发明设计人 ARTHUR E. HARMS;

    申请日2008-01-11

  • 分类号C07D401/04;A61K31/55;A61K31/551;A61K31/553;A61K31/554;A61P31/04;C07D215/233;C07D413/04;C07D417/04;

  • 国家 BR

  • 入库时间 2022-08-21 15:58:37

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