Synthesis of Halopyrazole Matrine Derivatives and Their Insecticidal and Fungicidal Activities

卤代吡唑类苦参碱衍生物的合成及其杀虫杀菌活性

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作者:Xingan Cheng, Huiqing He, Fangyun Dong, Chunbao Charles Xu, Hanhui Zhang, Zhanmei Liu, Xiaojing Lv, Yuehua Wu, Xuhong Jiang, Xiangjing Qin

Abstract

Matrine is a traditional botanical pesticide with a broad-spectrum biological activity that is widely applied in agriculture. Halopyrazole groups are successfully introduced to the C13 of matrine to synthesize eight new derivatives with a yield of 78-87%. The insecticidal activity results show that the introduction of halopyrazole groups can significantly improve the insecticidal activity of matrine on Plutella xylostella, Mythimna separata and Spodoptera frugiperda with a corrected mortality rate of 100%, which is 25-65% higher than matrine. The fungicidal activity results indicate that derivatives have a high inhibitory effect on Ceratobasidium cornigerum, Cibberella sanbinetti, Gibberrlla zeae and Collectot tichum gloeosporioides. Thereinto, 4-Cl-Pyr-Mat has the best result, with an inhibition rate of 23-33% higher than that of matrine. Therefore, the introduction of halogenated pyrazole groups can improve the agricultural activity of matrine.

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