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    • 1. 发明公开
    • PROCESS FOR PREPARING AN ORTHO-SUBSTITUTED 5-HALOPHENOL AND A SYNTHESIS INTERMEDIATE THEREOF
    • VERFAHRENFÜRDIE ZUBEREITUNG EINES ORTHO-SUBSTITUIERTEN 5-HALOPHENOLS UND SYNTHESEZWISCHENPRODUKT DARAUS
    • EP2574192A4
    • 2013-12-25
    • EP10851578
    • 2010-05-19
    • RHODIA CHINA CO LTDRHODIA OPERATIONS
    • MERCIER CLAUDEDE CAMPO FLORYANRIGHINI SEBASTIEN
    • C07C309/12C07C41/01C07C43/253
    • C07C303/28C07C41/26C07C303/30C07C309/66C07C43/23
    • A process for preparing a 5-halophenol, ortho-substituted by an electron-donating group, is described. Also described, is a process for preparing a sulphonic ester of an ortho-substituted phenol, which is the synthesis intermediate for the ortho-substituted 5-halophenol. The process for preparing a phenol ortho-substituted by an electron-donating group and protected in the form of a sulphonic ester can include reacting a phenol ortho-substituted by an electron-donating group with a sulphonylating agent in the presence of a Lewis acid. The process for preparing a 5-halophenol ortho-substituted by an electron-donating group can include a first step of preparing a phenol ortho-substituted by an electron-donating group and protected in the form of a sulphonic ester, as described above; a second step of halogenating the protected phenol intermediate obtained in the preceding step, in the position para to the electron-donating group; and a third step of deprotecting the sulphonic ester function to hydroxyl.
    • 描述了制备供电子基团邻位取代的5-卤代苯酚的方法。 还描述了一种制备邻取代苯酚的磺酸酯的方法,该取代苯酚是邻位取代的5-卤代苯酚的合成中间体。 制备供电子基团邻位取代的并以磺酸酯形式保护的苯酚的方法可以包括在路易斯酸存在下,使由供电子基团取代的苯酚与磺酰化剂反应。 制备供电子基团邻位取代的5-卤代苯酚的方法可以包括制备被供电子基团邻位取代的苯酚并以磺酸酯形式保护的第一步,如上所述; 在前述步骤中得到的被保护的酚中间体的供电子基团的对位卤化的第2工序; 和将磺酸酯官能团去保护成羟基的第三步。