摘要
[Objective] In order to improve the herbicidal activity of toxins III（methyl2-methyl-3,5-dinitrobenzoate） from Phoma herbarbum, its structure was optimized by derivatization. [Method] Sixteen novel title compounds were synthesized by nitration and acylation with o-toluic acid as a starting material. Their structures were confirmed by IR and1 H NMR. [Result] The herbicidal activity screening showed that the inhibition rate of J-L-59 against E. crusgalli roots was 93.7% at 100 μg/ml. The fresh weight efficacy of J-L-59 against A. theophrasti and A. retroflexus was 100%at 1 000 g a.i./hm^2 , and the ED50 value for A. retroflexus was 94.06 g a.i./hm^2 .[Conclusion] J-L-59 has higher herbicidal activity.
[目的]提高草茎点霉毒素III(2-甲基-3,5-二硝基苯甲酸甲酯)的除草活性,对其结构进行衍生优化。[方法]以邻甲基苯甲酸为起始原料,经硝化、酰化等反应合成了16个新的苯甲酸酯类化合物,其结构均通过IR和1H NMR确证,并对合成的化合物进行除草活性筛选。[结果]在100μg/ml时,J-L-59对稗草Echinochloa crusgalli根的抑制率为93.7%;活体盆栽试验结果表明,在有效成分1000 g/hm^2时,J-L-59对苘麻Abutilon theophrasti和反枝苋Amaranthus retroflexus的鲜重防效均达100%。毒力测定结果表示,J-L-59对反枝苋Amaranthus retroflexus的ED50值为有效成分94.06 g/hm^2。[结论]J-L-59有较高的除草活性。
基金
Supported by National Natural Science Foundation of China(31071746,31101466)~~
