3,4-二芳基-5-芳氧甲基异噁唑的合成
收稿日期: 2017-02-20
修回日期: 2017-04-07
网络出版日期: 2017-05-25
基金资助
国家自然科学基金（No.21272153）资助项目.
Synthesis of 3,4-Diaryl-5-aryloxymethyl Isoxazole Derivatives
Received date: 2017-02-20
Revised date: 2017-04-07
Online published: 2017-05-25
Supported by
Project supported by the National Natural Science Foundation of China (No. 21272153).
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.
关键词： 异噁唑衍生物; 溴代; 醚化; Suzuki偶联反应
蒋海芳 , 张敏 , 张丽 , 陈雅丽 , 朱宁 , 宋力平 , 邓红梅 . 3,4-二芳基-5-芳氧甲基异噁唑的合成[J]. 有机化学, 2017 , 37(9) : 2399 -2408 . DOI: 10.6023/cjoc201702026
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.
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