- Design, synthesis, herbicidal activity, and the molecular docking study of novel diphenyl ether derivatives as protoporphyrinogen IX oxidase inhibitors
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Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is an important herbicide target. In this study, a series of novel diphenyl ethers derivatives with 2-pyrrolidone structure were developed as PPO inhibitors. Thereinto, compound H7 (IC50 = 0.0262 mg/L) has better PPO enzyme inhibitory activity than commercial herbicide oxyfluorfen (IC50 = 0.0426 mg/L). Greenhouse herbicidal activity experiments exhibited that even under the condition of 37.5 g ai/ha, H7 still had excellent broad-spectrum herbicidal activity. Moreover, rice, peanut, and cotton had strong tolerance to H7 at 300 g ai/ha. Field trial showed that H7 had comparable herbicidal activity to oxyfluorfen. These experimental results indicated that H7 could be developed as a novel PPO Inhibitor candidate for weed control in the field.
- Fu, Ying,Gao, Shuang,Hu, Jia-Jun,Peng, Jian-Feng,Wang, Zhi-Xin,Ye, Fei,Yin, Min-Lei,Zhao, Li-Xia,Zou, Yue-Li
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- Triazole compound containing dioxolame and preparation method of intermediate of triazole compound
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The invention relates to a preparation method of a dioxolane-containing triazole compound and an intermediate thereof, and the method comprises the following steps: reacting a compound shown as a formula (V) with a compound shown as a formula (IV) in the presence of Lewis acid to prepare a compound shown as a formula (III); reacting the compound shown in the formula (III) with a compound shown in the formula (II) to prepare the compound shown in the formula (I). According to the technical scheme, a triazole group is introduced into 1H-1, 2, 4-triazole-1-acetic acid, generation of an isomer 1, 3, 4-triazole byproduct is avoided, the reaction yield is increased, and the method has the advantages of being simple and convenient in process route, few in reaction step, simple in process, low in production cost, environmentally friendly, green and safe; the post-treatment of the product only needs a simple solvent crystallization process, a nitric acid salifying method and a high-temperature distillation method do not need to be adopted, the requirements on equipment are reduced and the cost is reduced under the condition of improving the yield and content of the product, and the method is suitable for industrial production.
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- Method for synthesizing high-purity difenoconazole
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The invention discloses a method for synthesizing high-purity difenoconazole, which comprises the following steps: 1) carrying out acylation reaction on 3,4'-dichlorodiphenyl ether to obtain an intermediate I; 2) performing cyclization reaction on the intermediate I to obtain an intermediate II; 3) brominating 1,2,4-triazole to prepare a 1,2,-4-triazole bromide; 4) carrying out bromination reaction on the intermediate II and 1,2,4-triazole bromide to obtain an intermediate III and triazole, and carrying out condensation reaction on the intermediate III and 1,2,4-triazole under the action of potassium hydroxide to obtain a difenoconazole crude product; and 5) refining the difenoconazole crude product to obtain a difenoconazole refined product. The method is low in cost, high in quality andhigh in yield, dibromo and hydrolysis byproducts are hardly generated, and the product content and appearance quality of the difenoconazole refined product are improved.
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Paragraph 0003; 0004; 0006; 0017-0021
(2021/02/10)
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- Synthesis method and application of difenoconazole intermediate
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The invention provides a synthesis method and application of a difenoconazole intermediate. The synthesis method comprises the following steps: 1) carrying out acylation reaction on 2, 4-dichlorodiphenyl ether and acetyl chloride to prepare an intermediate I; 2) quenching the intermediate I with methanol to obtain an intermediate II; and 3) preparing the difenoconazole intermediate from the intermediate II and propylene glycol. The synthesis method is high in reaction speed and thorough in reaction, and the synthesized difenoconazole intermediate is used for preparing difenoconazole.
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Paragraph 0008; 0036-0037; 0040-0041; 0044-0045; 0048-0049
(2021/11/21)
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- FUNGICIDAL ALKYL-SUBSTITUTED 2-[2-CHLORO-4-(4-CHLORO-PHENOXY)-PHENYL]-1-[1,2,4]TRIAZOL-1-YL-ETHANOL COMPOUNDS
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The present invention relates to the use of alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.
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Page/Page column 4
(2013/03/26)
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- FUNGICIDAL SUBSTITUTED 1-{2-CYCLYLOXY-2-[2-HALO-4-(4-HALOGEN-PHENOXY)-PHENYL]-ETHYL}-1H-[1,2,4]TRIAZOLE COMPOUNDS
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The present invention relates to substituted 1-{2-cyclyloxy-2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-ethyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.
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Page/Page column 85
(2013/03/26)
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- TRIAZOLE COMPOUNDS CARRYING A SULFUR SUBSTITUENT
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The present invention relates to novel triazole compounds of the formulae I, II and IV to agricultural compositions containing them, to their use as fungicides and to intermediate compounds used in the method of producing them.
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Page/Page column 188
(2010/12/31)
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