新型含甲氨甲酰苯基烟酰脲类化合物的设计、合成及生物活性研究
收稿日期: 2014-04-22
修回日期: 2014-05-16
网络出版日期: 2014-06-11
Design, Synthesis and Bioactivities of Novel N-Methyl-carbamoylphenyl Nicotinoyl Ureas
Received date: 2014-04-22
Revised date: 2014-05-16
Online published: 2014-06-11
为了寻找新的农药先导化合物，以氯虫苯甲酰胺和2-氯烟酸结构为基础，依据生物合理设计思想引入酰脲活性基团，设计合成了12个结构新颖的烟酰脲类化合物. 其结构经1H NMR，13C NMR，IR及HRMS确认. 初步的生测活性测试结果表明，部分化合物对粘虫（Mythimna separata）具有较好的杀虫活性，在浓度为500 mg/L时，化合物5a，5g和5h处理的粘虫死亡率为100%；此外，部分化合物具有一定的除草活性，其中100 mg/L的化合物5f对稗草（Echinochloa crusgalli）根部生长抑制率为80%.
刘建华 , 李以名 , 毛达杰 , 杜晓华 . 新型含甲氨甲酰苯基烟酰脲类化合物的设计、合成及生物活性研究[J]. 有机化学, 2014 , 34(10) : 2140 -2145 . DOI: 10.6023/cjoc201404040
In order to look for new pesticidal leading compounds, 12 novel nicotinoyl ureas were designed and synthesized based on the structure fragments of chlorantraniliprole and 2-chloronicotinic acid according to the bio-rational design principle. The structures of all compounds have been confirmed by 1H NMR, 13C NMR, IR and HRMS techniques. The preliminary results of biological sceen indicated that some of the title compounds exhibited high insecticidal activities against Mythimna separate. At 500 mg/L, compounds 5a, 5g and 5h exhibited a insecticidal activity of 100%. In additional, some compounds showed herbicidal activities, such as 100 mg/L of compounds 5f inhibited 80% root growth against Echinochloa crusgalli.
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