3,4-二芳基-5-芳氧甲基异噁唑的合成

Synthesis of 3,4-Diaryl-5-aryloxymethyl Isoxazole Derivatives

由于异噁唑衍生物具有广泛的除草、杀虫和药物活性,其合成方法近年来一直引起关注.以3-芳基-5-溴甲基异噁唑为原料,经溴代、醚化、Suzuki偶联反应合成了一系列3,4-二取代芳基-5-芳氧甲基异噁唑化合物,初步的生物活性测试结果显示,部分化合物对粘虫显示出一定的杀虫活性.

Due to isoxazole derivatives possess a wide range of herbicidal, insecticidal and pharmacological activitives, the synthetic methodologies for preparation of isoxazole derivatives have drawn much attention in recent years. Herein, 3,4-diaryl-5-aryloxymethyl isoxazole derivatives were effectively synthesized from 3-aryl-5-（bromomethyl）isoxazole via consecutive bromination, etherification, followed by Suzuki coupling reaction catalyzed by Pd（PPh3）2Cl2. Preliminary bioassay data showed that some of the title compounds exhibited certain insecticidal activities against Oriental armyworm.