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    • 1. 发明授权
    • Process for producing 4-substituted benzopyran derivatives
    • 制备4-取代苯并吡喃衍生物的方法
    • US06608217B2
    • 2003-08-19
    • US10255099
    • 2002-09-26
    • Takeo KomataMasaki FujiwaraTakanao TaruiYusuke SaitoHiroshi Minesaki
    • Takeo KomataMasaki FujiwaraTakanao TaruiYusuke SaitoHiroshi Minesaki
    • C07D31104
    • C07D311/58C07C45/46C07C45/673C07C49/84C07C49/825
    • The present invention relates to a first process for producing a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-carboxylic acid. The first process includes the steps of (a) reacting a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-one with a perfluoroalkanesulfonic acid anhydride in the presence of a base, thereby obtaining a perfluoroalkanesulfonic 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H- 1-benzopyran-4-yl ester; and (b) reacting the benzopyranyl ester with carbon monoxide in the presence of a palladium complex compound and a base, thereby obtaining the carboxylic acid. The present invention further relates to a second process for producing a 2-hydroxy-5-(perfluoroalkyl) acetophenone, which can be a raw material for producing the carboxylic acid. The second process includes the steps of (c) reacting a 4-(perfluoroalkyl)alkoxybenzene with acetic anhydride or an acyl halide in the presence of a Lewis acid, thereby obtaining a 2-alkoxy-5-(perfluoroalkyl)acetophenone; and (d) dealkylating the 2-alkoxy-5-(perfluoroalkyl) acetophenone by a dealkylating agent.
    • 本发明涉及生产2,2-双(氟甲基)-6-(全氟烷基)-2H-1-苯并吡喃-4-羧酸的第一种方法。 第一种方法包括以下步骤:(a)在碱的存在下使2,2-双(氟甲基)-6-(全氟烷基)-2H-1-苯并吡喃-4-酮与全氟烷基磺酸酐反应,从而得到 全氟烷基磺酸2,2-双(氟甲基)-6-(全氟烷基)-2H-苯并吡喃-4-基酯; 和(b)在钯络合物和碱的存在下使苯并吡喃基酯与一氧化碳反应,由此得到羧酸。 本发明还涉及可用作生产羧酸的原料的2-羟基-5-(全氟烷基)苯乙酮的制备方法。 第二种方法包括以下步骤:(c)在路易斯酸存在下使4-(全氟烷基)烷氧基苯与乙酸酐或酰卤反应,由此得到2-烷氧基-5-(全氟烷基)苯乙酮; 和(d)通过脱烷基化剂使2-烷氧基-5-(全氟烷基)苯乙酮脱烷基化。