3-芳基-4-芳胺甲基异噁唑衍生物的合成及其生物活性初探  

Synthesis and Preliminary Exploration of Biological Activity of 3-Aryl-4-arylamine Methyl Isoxazoles

作　　者：李倩倩 吴中梅 张敏[1] 张一平 周英楷 邓红梅[3] 宋力平[1,2] Li Qianqian;Wu Zhongmei;Zhang Min;Zhang Yiping;Zhou Yingkai;Deng Hongmei;Song Liping(Department of Chemistry,College of Science,Shanghai University,Shanghai 200444;Key Laboratory of Organofluorine Chemistry,Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences,Shanghai 200032;Laboratory for Microstructures,Shanghai University,Shanghai 200444)

机构地区：[1]上海大学理学院化学系,上海200444 [2]中国科学院上海有机化学研究所有机氟化学重点实验室,上海200032 [3]上海大学微结构重点实验室,上海200444

出　　处：《有机化学》2020年第7期2108-2113,共6页Chinese Journal of Organic Chemistry

基　　金：中国科学院上海有机化学研究所有机氟化学重点实验室资助项目.

摘　　要：异噁唑衍生物由于其良好的生物活性一直受到有机合成化学家的关注,例如异噁唑衍生物具有杀虫、杀菌等生物活性.以3-芳基4-异噁唑甲酸乙酯为原料,经还原、溴化、取代反应合成了一系列3-芳基-4-芳胺甲基异噁唑衍生物,目标化合物结构经过1 H NMR、13C NMR、HRMS鉴定.初步的生物活性测试结果显示,部分化合物对蚜虫和粘虫具有较好的抑制率.The synthesis of isoxazole derivatives has been paid much attention by organic synthetic chemists because isoxazoles usually exhibit good biological activity such as insecticidal and bactericidal activity.In this study,a series of 3-aryl-4-arylamine methyl isoxazole derivatives were synthesized from ethyl 3-arylisoxazole-4-carboxylate by reduction,bromination and substitution reaction.The synthesized compounds were identified by 1 H NMR,13C NMR and HRMS,and the preliminary bioactivity test results showed that some compounds obtained had good inhibitory effects anainst aphids and armyworms.

关 键 词：异噁唑衍生物 合成 芳胺甲基 生物活性 

分 类 号：O626.24[理学—有机化学]