| 三氟羧草醚类似物的合成及除草活性 |
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| 引用本文： | 赵卓然,李佳康,李占斌,陈雨,黄玉乾,李文琪,姬志勤,魏少鹏.三氟羧草醚类似物的合成及除草活性[J].农药学学报,2022,24(3):465-473. |
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| 作者姓名： | 赵卓然 李佳康 李占斌 陈雨 黄玉乾 李文琪 姬志勤 魏少鹏 |
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| 作者单位： | 1.西北农林科技大学 植物保护学院，陕西 杨凌 712100 |
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| 基金项目： | 国家自然科学基金(31872011). |
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| 摘 要： | 以2,5-二羟基苯甲酸甲酯和三氟羧草醚为起始原料，设计合成了3个系列20个新的三氟羧草醚类似物，通过核磁共振氢谱、碳谱对其结构进行了表征。分别采用小杯法和室内盆栽法测定了目标化合物的除草活性。结果表明，化合物 III-02 5-(2-氯-4-三氟甲基苯氧基)-2-硝基苯甲酸-(6-甲基苯并噻唑-2-基)酯]对单子叶杂草的除草活性明显高于对照药剂三氟羧草醚，其对稗草Echinochloa crusgalli和马唐Digitaria sanguinalis根茎生长的EC50值分别为2.03、0.93 μg/mL和1.49、0.52 μg/mL；在有效成分100 g/hm2的施药剂量下，化合物 III-02 对单子叶杂草稗草、马唐及狗尾草Setaria viridis的防治效果均在85%以上，明显高于三氟羧草醚，对阔叶杂草马齿苋Portulaca oleracea、反枝苋Amaranthus retroflexus及苘麻Abutilon theophrasti的防治效果可达100%。初步构效关系表明，2-硝基苯甲酰衍生物的除草活性明显优于其2-甲氧基衍生物，三氟羧草醚苯甲酸酯衍生物对单子叶杂草的除草活性明显高于其苯甲酰胺衍生物。
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| 关 键 词： | 三氟羧草醚 类似物 合成 除草活性 构效关系 |
| 收稿时间： | 2021-11-03 |
Synthesis and herbicidal activity of acifluorfen analogues |
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| Affiliation: | 1.College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi Province, China2.Shaanxi Province Key Laboratory Research & Development on Botanical Pesticides, Yangling 712100, Shaanxi Province, China |
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| Abstract: | Three series of twenty new acifluorfen analogues were designed and synthesized using methyl 2,5-dihydroxybenzoate and acifluorfen as starting materials. Their structures were characterized by 1H NMR and 13C NMR. The herbicidal activities of the compounds were determined by methods of petri dish and greenhouse potted. The results showed that the herbicidal activity of compound III-02 6-methylbenzod]thiazol-2-yl 5-(2-chloro-4-(trifluoromethyl)phenoxy)-2-nitrobenzoate] against monocotyledonous weeds was significantly higher than that of acifluorfen, and its EC50 values were 2.03, 0.93 μg/mL and 1.49, 0.52 μg/mL against the roots and stems of Echinochloa crusgalli and Digitaria sanguinalis, respectively. Additionally, at the dosage of 100 g a.i./ha, the efficacy of compound III -02 against monocotyledonous weeds E. crusgalli, S. sanguinalis and Setaria viridis was above 85%, which was significantly higher than that of acifluorfen, and a 100% control effect on broadleafs Portulaca oleracea, Amaranthus retroflexus and Abutilon theophrasti. The structure-activity relationship showed that the herbicidal activity of 2-NO2 benzoyl derivatives was significantly higher than that of 2-OCH3 analogues, and the herbicidal activity of acifluorfen benzoate derivatives against monocotyledons was significantly higher than that of benzamide derivatives. |
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