| 2-氰基-3-甲硫基-3-取代甲氨基丙烯酸酯类化合物的合成及其除草活性 |
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| 引用本文： | 高颖,邹小毛,郁丽敏,许寒,刘斌,朱有全,胡方中,杨华铮. 2-氰基-3-甲硫基-3-取代甲氨基丙烯酸酯类化合物的合成及其除草活性[J]. 中国化学, 2006, 24(4): 521-526. DOI: 10.1002/cjoc.200690100 |
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| 作者姓名： | 高颖 邹小毛 郁丽敏 许寒 刘斌 朱有全 胡方中 杨华铮 |
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| 作者单位： | State Key Laboratory of Elemento-organic Chemistry, Research Institute of Elemento-organic Chemistry, Nankai University, Tianjin 300071, China |
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| 基金项目： | Project supported by the National Key Project for Basic Research （No. 2003CB114400）, Research Fund for the Doctoral Program of Higher Education in China （No. 20020055022） and the National Natural Science Foundation of China （No. 20372040）. |
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| 摘 要： | A series of 2-cyano-3-methylthio-3-substituted methylaminoacrylates were synthesized as herbicidal inhibitors of photosystem Ⅱ （PSⅡ） electron transport, in order to estimate the effect of fluorine atom, pyridyl group, chirality and ester chain on activity. The important intermediate 2-fluoro-5-aminomethylpyridine was synthesized with high yield. The bioassay results showed that most of rifle compounds had high herbicidal activity in postemergence treatment. The introduction of an a-methyl into the 3-substituted methylamino could improve the activity notably. The replacement of hydrogen by chlorine or fluorine group and phenyl by pyridyl group showed different effects, and at the same time, the ester chain affected the activity too.
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| 关 键 词： | 合成 除草活性 氟 手性 2-蓝色-3-甲基硫代-3-取代甲基 氨基丙烯酸脂 光合体系 抑制剂 |
| 收稿时间： | 2005-08-25 |
| 修稿时间： | 2005-08-252005-12-29 |
Synthesis and Herbicidal Activity of 2-Cyano-3-methylthio-3-substituted Methylaminoacrylates |
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| GAO Ying, ZOU Xiao-Mao, YU Li-Min,XU Han, LIU Bin, ZHU You-Quan, HU Fang-Zhong, YANG Hua-Zheng. Synthesis and Herbicidal Activity of 2-Cyano-3-methylthio-3-substituted Methylaminoacrylates[J]. Chinese Journal of Chemistry, 2006, 24(4): 521-526. DOI: 10.1002/cjoc.200690100 |
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| Authors: | GAO Ying ZOU Xiao-Mao YU Li-Min XU Han LIU Bin ZHU You-Quan HU Fang-Zhong YANG Hua-Zheng |
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| Affiliation: | State Key Laboratory of Elemento-organic Chemistry, Research Institute of Elemento-organic Chemistry, Nankai University, Tianjin 300071, China |
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| Abstract: | A series of 2‐cyano‐3‐methylthio‐3‐substituted methylaminoacrylates were synthesized as herbicidal inhibitors of photosystem II (PSII) electron transport, in order to estimate the effect of fluorine atom, pyridyl group, chirality and ester chain on activity. The important intermediate 2‐fluoro‐5‐aminomethylpyridine was synthesized with high yield. The bioassay results showed that most of title compounds had high herbicidal activity in postemergence treatment. The introduction of an α‐methyl into the 3‐substituted methylamino could improve the activity notably. The replacement of hydrogen by chlorine or fluorine group and phenyl by pyridyl group showed different effects, and at the same time, the ester chain affected the activity too. |
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| Keywords: | 2-cyanoacrylates herbicidal activity fluorine chirality substituted pyridylmethylamino |
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