| 草茎点霉毒素Ⅲ衍生物的合成与除草活性 |
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投稿时间：2015-06-19
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| 引用本文：纪明山,刘欣,高云云,等.草茎点霉毒素Ⅲ衍生物的合成与除草活性[J].农药学学报,2015,17(5):520-529. |
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| 基金项目:草茎点霉毒素Ⅲ对鸭跖草致病机理研究;国家自然科学基金项目(31071746,31101466). |
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| 中文摘要:为了提高草茎点霉毒素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。以邻甲基苯甲酸为起始原料,经硝化、酯化等反应合成了34个新的苯甲酸酯类化合物,其结构均通过IR、1H NMR和GC-MS确证。杂草种子萌发试验结果表明,目标化合物对供试杂草根的抑制率明显高于茎,在100 μg/mL时,4-15、4-16和4-26对反枝苋Amaranthus retroflexus根的抑制率分别为92.8%、92.0%和87.4%,有较显著的除草活性;活体盆栽试验结果表明,在有效成分1 000 g/hm2时,4-1对马唐 Digitaria sanguinalis和反枝苋A. retroflexus的鲜重防效均达100%,有较高的除草活性;毒力测定结果表明,4-1 对马唐D.sanguinalis的ED50值为有效成分94.89 g/hm2。 |
| 中文关键词:草茎点霉 苯甲酸酯 合成 除草活性 |
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| Synthesis and herbicidal activity evaluation of toxins Ⅲ from Phoma herbarbum derivatives |
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| Abstract:In order to improve the herbicidal activity of toxins Ⅲ (2-methyl-3, 5-dinitrobenzoic acid methyl ester) from Phoma herbarbum, their structure were optimized by derivation. 34 novel title compounds were synthesized by nitration, esterification starting from o-toluic acid as the starting material. Their structure were characterized by IR, 1H NMR and GC-MS. The screening of the herbicidal activity showed that the inhibition rates of the target compounds on the roots of weed were higher than that of the shoots. The inhibition rates of 4-15, 4-16 and 4-26 against Amaranthus retroflexus root were 92.8%, 92.0% and 87.4% at 100 μg/mL, respectively, which demonstrated significant herbicidal activity. The fresh weight efficacy of 4-1 against Digitaria sanguinalis and A.sretroflexus was 100% at 1 000 g a.i./hm2, which illustrated high herbicidal activity. The ED50 value for D. sanguinalis was 94.89 g a.i./hm2. |
| Key words:Phoma herbarbum benzoic esters synthesis herbicidal activity |
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