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PROCESS FOR PREPARING AN ORTHO-SUBSTITUTED 5-HALOPHENOL AND A SYNTHESIS INTERMEDIATE THEREOF

机译:制备被邻位取代的5-卤代酚及其合成中间体的方法

摘要

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.
机译:描述了制备被供电子基团邻位取代的5-卤代苯酚的方法。还描述了制备邻取代的苯酚的磺酸酯的方法,该磺酸取代酯是邻取代的5-卤代苯酚的合成中间体。制备被供电子基邻取代的苯酚并以磺酸酯形式保护的苯酚的方法可包括在路易斯酸存在下,使经供电子基邻取代的苯酚与磺化剂反应。如上所述,制备被供电子基邻位取代的5-卤代苯酚的方法可包括第一步,制备被供电子基邻位取代且以磺酸酯形式被保护的酚,如上所述。第二步是在给电子基团的对位卤化在前一步中得到的被保护的酚中间体。第三步是使磺酸酯官能团脱保护成羟基。

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