Methods and systems for forming boronic acids and intermediates thereof
    1.
    发明授权
    Methods and systems for forming boronic acids and intermediates thereof 有权
    形成硼酸的方法和体系及其中间体

    公开(公告)号:US09145428B2

    公开(公告)日:2015-09-29

    申请号:US13618128

    申请日:2012-09-14

    摘要: Methods for forming boronic acids, and intermediates thereof, are disclosed. The method may include mixing a 1-chloro-2-substituted-3-fluorobenzene starting material with an alkyllithium in a first reactor to form a reaction mixture. The 1-chloro-2-substituted-3-fluorobenzene starting material may react with the alkyllithium to form a lithiated intermediate. The reaction mixture may be continuously transferred to a second reactor and a borate may be continuously introduced to form a boronate. The boronic acids may be formed by treating the boronate with aqueous potassium hydroxide followed by acidification. Such methods may provide continuous formation of the boronic acids and may reduce an amount of a reactive intermediate present during processing as well as cycle times. Systems for forming the boronic acids are also disclosed.

    摘要翻译: 公开了形成硼酸的方法及其中间体。 该方法可以包括在第一反应器中将1-氯-2-取代-3-氟苯原料与烷基锂混合以形成反应混合物。 1-氯-2-取代-3-氟苯原料可与烷基锂反应形成锂化中间体。 反应混合物可以连续转移到第二反应器中,并且可以连续引入硼酸盐以形成硼酸酯。 硼酸可以通过用氢氧化钾水溶液处理硼酸盐然后酸化而形成。 这样的方法可以提供连续形成的硼酸并且可以减少在加工期间和循环时间内存在的反应性中间体的量。 还公开了用于形成硼酸的体系。

    METHODS AND SYSTEMS FOR FORMING BORONIC ACIDS AND INTERMEDIATES THEREOF
    2.
    发明申请
    METHODS AND SYSTEMS FOR FORMING BORONIC ACIDS AND INTERMEDIATES THEREOF 有权
    形成硼酸的方法和系统及其中间体

    公开(公告)号:US20130066115A1

    公开(公告)日:2013-03-14

    申请号:US13618128

    申请日:2012-09-14

    IPC分类号: C07F5/02 B01J19/00

    摘要: Methods for forming boronic acids, and intermediates thereof, are disclosed. The method may include mixing a 1-chloro-2-substituted-3-fluorobenzene starting material with an alkyllithium in a first reactor to form a reaction mixture. The 1-chloro-2-substituted-3-fluorobenzene starting material may react with the alkyllithium to form a lithiated intermediate. The reaction mixture may be continuously transferred to a second reactor and a borate may be continuously introduced to form a boronate. The boronic acids may be formed by treating the boronate with aqueous potassium hydroxide followed by acidification. Such methods may provide continuous formation of the boronic acids and may reduce an amount of a reactive intermediate present during processing as well as cycle times. Systems for forming the boronic acids are also disclosed.

    摘要翻译: 公开了形成硼酸的方法及其中间体。 该方法可以包括在第一反应器中将1-氯-2-取代-3-氟苯原料与烷基锂混合以形成反应混合物。 1-氯-2-取代-3-氟苯原料可与烷基锂反应形成锂化中间体。 反应混合物可以连续转移到第二反应器中,并且可以连续引入硼酸盐以形成硼酸酯。 硼酸可以通过用氢氧化钾水溶液处理硼酸盐然后酸化而形成。 这样的方法可以提供连续形成的硼酸并且可以减少在加工期间和循环时间内存在的反应性中间体的量。 还公开了用于形成硼酸的体系。