4-((3-甲氧基苯基)氨基甲酰基)苯硼酸合成研究  

Synthesis of ( 4-(( 3-methoxyphenyl) carbamoyl) phenyl) boronic acid

作　　者：管洪素 胡馨驰 余航 

机构地区：[1]贵州省分析测试研究院,贵州贵阳550002

出　　处：《贵州科学》2018年第1期91-93,共3页Guizhou Science

摘　　要：4-((3-甲氧基苯基)氨基甲酰基)苯硼酸是合成多种二芳基酰胺衍生物的重要中间体。该系列化合物具有抑制CCR5受体的生物活性。以对甲基苯硼酸为起始原料,经过氧化,酰氯化,酰胺化三步反应首次合成了目标化合物,其结构经1H NMR确证。该方法原料廉价易得,操作简便易控且收率较高,反应总收率80.8%。（ 4-（（ 3-methoxyphenyl） carbamoyl） phenyl） boronic acid is an important intermediate for the synthesis of various diarylamide derivatives which have the biological activity of inhibiting the CCR5 receptor. In this study,the target compound was synthesized through oxidation,chloridization and amidation with p-tolylboronic acid as the starting material. Then its structure was confirmed by1 H NMR. This method has the advantages including cheap and easy-to-get raw materials,easy to operate,and high yield. The total yield reached up to 80. 8%.

关 键 词：苯硼酸 CCR5受体 对甲基苯硼酸 合成 

分 类 号：O625.55[理学—有机化学]