酪氨酸酶催化对位取代苯酚和芳香胺的反应及其意义

用固定化酪氨酸酶催化4－取代烷基或烷氧基单酚类化合物的氧化反应得到相 应的4-取代邻苯醌，这类邻苯醌能和芳香胺发生迈克尔加成反应，烷基或烷氧基从 醌环4位上脱落，得到三取代胺的化合物。将抗炎药布洛芬引入到单酚的苯环4位上 ，在酪氨酸酶和芳香胺同时存在的条件下，也得到脱布洛芬的加成取代产物，显示 4－羟基布洛芬苯酚酯可作为布洛芬药物载体。

Tyrosinase Catalyzed Reaction of 4-Substituted-phenol wth Aryl Amine

4-Substituted-l, 2-benzoquinones were obtained from monophenolization by the immobilized tyrosinase. The 4-substituted-1,2- benzoquinones react with aryl amines to afford Michael addition products 3a ~ 3c. In these reactions the alkyl and alkyloxy groups in the 4-position are displaced by an arylamino-group. A novel prodrug of brufen (4-isobutyl-a-methylphenylacetic acid) was designed and synthesized. According to the tyrosinase-mediated drug release, it has been shown that it acts in the desired manner.