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Iodine-mediated oxidative cyclization for one pot synthesis of new 8-hydroxyquinaldine derivatives containing a N-phenylpyrazole moiety as pesticidal agents
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-09-01 , DOI: 10.1016/j.bmcl.2018.08.041
Ting Xu , Xiaoguang Wang , Qian Zhang , Jiangping Fan , Liu Liu , Mingzhu Liu , Haojie Zhang , Jing Li , Yong Guo

In continuation of our research aimed at discovery and development of new pesticidal agents, a series of new 8-hydroxyquinaldine derivatives containing a N–phenylpyrazole moiety were prepared and their structures were characterized by 1H NMR, IR, ESI-MS and mp. Meanwhile, an efficient way of using iodine-mediated oxidative cyclization for one pot synthesis of these 8-hydroxyquinaldine derivatives containing a N–phenylpyrazole moiety was developed. The bioassay showed that compounds 8g and 9f exhibited potent pesticidal activities against both Mythimna separata Walker and Plutella xylostella Linnaeus. The structure–activity relationships were also discussed.



中文翻译:

碘介导的氧化环化反应,用于一锅合成含有N-苯基吡唑部分作为杀虫剂的新型8-羟基奎纳衍生物

在我们旨在发现和开发新农药的研究的继续中,制备了一系列含有N-苯基吡唑部分的新型8-羟基奎纳衍生物,并通过1 H NMR,IR,ESI-MS和mp对其结构进行了表征。同时,开发了一种有效的方法,利用碘介导的氧化环化反应一锅合成这些含有N-苯基吡唑部分的8-羟基奎纳丁衍生物。生物测定表明,化合物8g9f对分离的Mythimna separata Walker和Plutella xylostella Linnaeus均显示出有效的杀虫活性。还讨论了构效关系。

更新日期:2018-09-01
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