2,4,6- OR 2,6-ALKOXYPHENYL DIALKYLPHOSPHINE, TETRAFLUOROBORATE, PREPARATION METHOD AND USE THEREOF
    1.
    发明公开
    2,4,6- OR 2,6-ALKOXYPHENYL DIALKYLPHOSPHINE, TETRAFLUOROBORATE, PREPARATION METHOD AND USE THEREOF 有权
    2,4,6-或2,6-烷氧基苯基二烷基膦,四氟硼酸盐,制备方法及其用途

    公开(公告)号:EP2492274A1

    公开(公告)日:2012-08-29

    申请号:EP09850497.0

    申请日:2009-12-21

    摘要: The current invention relates to the structure, synthesis of dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate, as well as its applications in the palladium catalyzed carbon-chlorine bond activation for Suzuki coupling reactions and carbon-nitrogen bond formation reactions. The dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate could coordinate with the palladium catalyst to activate the inert carbon-chlorine bond highly selectively and catalyze Suzuki coupling reaction with arylboronic acid or carbon-nitrogen bond formation reaction with organic amines. The current invention uses only one step to synthesize dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate is stable in the air. Compared with known synthetic routes of ligands used in activating carbon-chlorine bonds, the method of current invention is short, easy to operate. Moreover, with this type of ligands, the Suzuki coupling products of optically active chlorolactones and arylboronic acids would maintain their configuration and optical purity.

    摘要翻译: 本发明涉及二烷基(2,4,6-或2,6-烷氧基苯基)膦或其四氟硼酸盐的结构,合成,以及其在用于Suzuki偶联反应和碳的钯催化的碳 - 氯键活化中的应用 - 氮键形成反应。 二烷基(2,4,6-或2,6-烷氧基苯基)膦或其四氟硼酸盐可与钯催化剂配位以高度选择性地活化惰性碳 - 氯键并催化与芳基硼酸的Suzuki偶联反应或碳 - 氮键形成 与有机胺反应。 本发明仅使用一个步骤来合成二烷基(2,4,6-或2,6-烷氧基苯基)膦,并且其四氟硼酸盐在空气中稳定。 与已知的用于活化碳 - 氯键的配体的合成路线相比,本发明的方法短暂且易于操作。 此外,对于这种类型的配体,光学活性氯内酯和芳基硼酸的Suzuki偶联产物将保持其构型和光学纯度。