TWI646894B - Agrochemical composition, method for its preparation and the use thereof - Google Patents
Agrochemical composition, method for its preparation and the use thereof Download PDFInfo
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- A—HUMAN NECESSITIES
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- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
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Abstract
本發明提供一種農用化學品組成物,該組成物含有依普同及最少一種來自通式(I)化合物的巨環內酯(macrolide)化合物:
Description
本發明有關一種農用化學品組成物,尤其是殺線蟲組成物。本發明亦有關調製上述農用化學品組成物的方法及其防治線蟲的功用。 The invention relates to an agrochemical composition, in particular a nematicidal composition. The invention also relates to a method of modulating the above-described agrochemical composition and its function of controlling nematodes.
線蟲是微小的迴蟲,一般為水生、三胚層、不分節、兩側對稱,且無色、透明、大多為雙性、呈蠕蟲狀(亦有些形狀腫脹)。有人指出線蟲為最多形態的動物,而現時為止,僅約3%線蟲種類已有深入研究。 The nematode is a tiny worm, usually aquatic, three germ layers, undivided, bilaterally symmetrical, and colorless, transparent, mostly bisexual, wormlike (also some shape swelling). It has been pointed out that nematodes are the most morphological animals, and only about 3% of nematode species have been studied intensively.
植物寄生線蟲一般以植物的根部及嫩芽為食。線蟲可分為外寄生,以寄生植物的外部為生;或內寄生,於寄生植物內部生存/進食。寄生線蟲可分為遷移性或固著性,對多種農藝及園藝作物造成嚴重植物產量限制。嚴重感染內部寄生線蟲如根結或胞囊線蟲可導致收成損失10%至50%。估計全球每年因植物寄生線蟲而引致的作物損失達800億元。 Plant parasitic nematodes generally feed on the roots and shoots of plants. Nematodes can be divided into ectoparasites, living on the outside of parasitic plants; or endoparasites, living/feeding inside parasitic plants. Parasitic nematodes can be classified as migratory or sessile, causing severe plant yield limitations on a variety of agronomic and horticultural crops. Severe infection with internal parasitic nematodes such as root knots or cyst nematodes can result in harvest losses of 10% to 50%. It is estimated that the annual crop loss caused by plant parasitic nematodes reaches 80 billion yuan.
商業上最為熟知的植物寄生線蟲如下: The most commercially known plant parasitic nematodes are as follows:
根瘤線蟲(Meloidogyne);根瘤線蟲(Root-knot nematode) Meloidogyne ; Root-knot nematode
根腐線蟲(Pratylenchus);腐線蟲(Lesion nematode) Root rot nematode (Pratylenchus) ; rot nematode (Lesion nematode)
胞囊線蟲(Heterodera);胞囊線蟲(Cyst nematode) Heterodera ; Cyst nematode
黃金線蟲(Globodera);胞囊線蟲(Cyst nematode) Globodera ; Cyst nematode
莖線蟲(Ditylenchus);莖線蟲(Stem and bulb nematode) Ditylenchus ; Stem and bulb nematode
穿刺線蟲(Tylenchulus);柑橘線蟲(Citrus nematode) Tylenchulus ; Citrus nematode
劍線蟲(Xiphinema);劍線蟲(Dagger nematode) Xiphinema ; Dagger nematode
穿孔線蟲(Radopholus);穿孔線蟲(Burrowing nematode) Radopholus ; Burrowing nematode
腎形線蟲(Rotylenchulus);腎形線蟲(Reniform nematode) Rotylenchulus ; Reniform nematode
螺旋線蟲(Helicotylenchus);螺旋線蟲(Spiral nematode) Helicover (Helicotylenchus) ; Spiral nematode
刺線蟲(Belonolaimus);針刺線蟲(Sting nematode)。 Nematode (Belonolaimus) ; Sting nematode.
線蟲是嚴重的蟲患,防治線蟲寄生的方法於現代集約式農業中對增加作物產量屬重要。現有線蟲的防治方法非常有限。土壤熏蒸劑及有效的非燻蒸性殺線蟲劑(尤其氨基甲酸鹽及有機磷化合物)日漸受到規管,此乃由於其對用戶、使用者及環境構成潛在的不良影響。其他有效減少植物寄生線蟲數目的方法,如以蒸汽處理病土從而進行加熱,對本領域一般或廣泛應用而言,不但過程繁複,而且成本高昂。 Nematodes are serious pests, and the method of controlling nematode parasites is important for increasing crop yields in modern intensive agriculture. Existing methods for controlling nematodes are very limited. Soil fumigants and effective non-fumigation nematicides (especially carbamates and organophosphorus compounds) are increasingly regulated due to their potential adverse effects on users, users and the environment. Other methods for effectively reducing the number of plant-parasitic nematodes, such as steaming the soil for heating, are not only cumbersome but also costly for general or wide-area applications in the art.
若干種子處理方法,如使用阿巴汀作為殺線蟲藥,可有效地保護幼苗根部免受植物寄生線蟲等各種植物害蟲侵害。與受阿巴汀保護的植物相比,未受保護的根部會出現萎縮,如有根瘤線蟲(root-knot nematodes)(根瘤線蟲,Meloidogyne spp.)更會出現嚴重的根瘤。嫩芽的明顯高度及乾重差異也反映著此等土壤下的分別。然而,種子處理的防治線蟲效用一般僅持續較短時間。 Several seed treatment methods, such as the use of abatatin as a nematicide, can effectively protect the roots of seedlings from various plant pests such as plant parasitic nematodes. Unprotected roots are atrophied compared to plants protected by Abatatin, and severe root nodules are more likely to occur in root-knot nematodes (Meloidogyne spp.). The difference in the height and dry weight of the shoots also reflects the difference in these soils. However, the efficacy of seed treatment for controlling nematodes generally lasts only for a short period of time.
因此,行業非常需要改良的殺線蟲組成物和防治線蟲以及其他植物害蟲及病原體的方法。如處理效果能長期維持,則更為有用。 Therefore, there is a great need in the industry for improved nematicidal compositions and methods for controlling nematodes and other plant pests and pathogens. It is more useful if the treatment effect can be maintained for a long time.
現時發現一種改良的農用化學品組成物,可用依普同混合最少一種巨環內酯(macrolide)化合物調製而成。 An improved agrochemical composition has now been found which can be prepared by mixing at least one macrolide compound.
因此,第一方面,本發明提供一種農用化學品組成物,含有依普同及最少一種來自通式(I)化合物的巨環內酯(macrolide)化合物:
令人意外的是,發現混合依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物會產生協同作用及更有效防治線蟲及其他植物害蟲及病原體。此組合對防治如蕃茄、胡椒、青瓜、蜜瓜、咖啡豆及大豆等作物有非常高的活性。 Surprisingly, it has been found that a mixture of epoxigen and at least one macrolide compound from the compounds of formula (I) and (II) produces synergistic effects and is more effective in controlling nematodes and other plant pests and pathogens. This combination has a very high activity against crops such as tomatoes, peppers, cucumbers, melons, coffee beans and soybeans.
本文所指的「協同」於此方面並非限於理解為組合的殺蟲作用,更指與單獨使用依普同及巨環內酯(macrolide)化合物相比,組合的其他有用特性。例如:擴大殺蟲譜的範圍至其他害蟲,如抗藥性病原菌;減少巨環內酯(macrolide)化合物的用量或以根據本發明按單獨使用無效的依普同及巨環內酯(macrolide)用量調製組成物,控制目標害蟲;提高作物的安 全性;提高生產質量(如含更高營養成分或油分、較優質纖維、更長的保質期、減少產品有毒成份如黴菌毒素、減少任何殘餘物或不良成份含量或更易於消化);提升抵受不合適溫度、乾旱或水中的鹽含量的能力;提升同化速度,如養分吸收、水分吸收及光合作用;有利的作物特性,如改變葉面面積、抑制植物生長、增加產量、有利的種子形狀/種子厚度或發芽特性、改變腐生或附生植物的依附、減少老化、增加植物防禦素的產生、加快植物成熟、花組增加、減少棉鈴落下及破損、更能吸引益蟲及捕食者、增加花粉傳播、減低對鳥類的吸引力。 The term "synergistic" as used herein is not limited to the understanding of the combined insecticidal action, but rather refers to other useful properties of the combination compared to the use of the ippro and macrolide compounds alone. For example: expanding the range of insecticidal spectrum to other pests, such as drug-resistant pathogens; reducing the amount of macrolide compounds or using the amount of lysine and macrolide that are ineffective according to the invention. Modulate the composition, control the target pests; increase the safety of the crop Improve the quality of production (such as containing higher nutrients or oils, higher quality fiber, longer shelf life, reducing product toxic ingredients such as mycotoxins, reducing any residue or undesirable ingredients or easier to digest); Ability to inappropriate salt, drought or salt content in water; increase assimilation rate, such as nutrient uptake, water uptake and photosynthesis; favorable crop characteristics such as changing leaf area, inhibiting plant growth, increasing yield, favorable seed shape / Seed thickness or germination characteristics, change the attachment of saprophytic or epiphytic plants, reduce aging, increase the production of plant defensins, accelerate plant maturation, increase the number of flower groups, reduce the falling and damage of cotton bolls, attract more beneficial insects and predators, and increase pollen transmission. Reduce the attraction of birds.
本發明的農用化學品組成物有效防治線蟲及其他植物害蟲及病原體,包括於蕃茄、胡椒、青瓜、咖啡豆及大豆等作物的南方根瘤線蟲(Meloidogyne incognita)及爪哇根瘤線蟲(Meloidogyne javanica)。 The agrochemical composition of the present invention is effective for controlling nematodes and other plant pests and pathogens, including Meloidogyne incognita and Meloidogyne javanica in crops such as tomatoes, peppers, cucumbers, coffee beans and soybeans.
本發明的組成物含有依普同。依普同為化合物3-(3,5-dichlorophenyl)-N-isopropyl-2,4-dioxoimidazolidine-1-carboxamide的通用名稱。依普同首次出現於US 3,755,350,作為殺真菌劑,特別防治翦股穎草的幣斑病、褐斑病、葉斑病。此殺真菌劑現有的藥證亦包括防治多種於草坪、商用盆景、蔬菜、果樹的葉部及土壤疾病,以及控制出現於花生的菌核病。依普同作為殺線蟲劑的效用載於EP 1 941 798。 The composition of the present invention contains the same. The common name of the compound 3-(3,5-dichlorophenyl)-N-isopropyl-2,4-dioxoimidazolidine-1-carboxamide. Yiputong first appeared in US 3,755,350 as a fungicide, especially for the prevention of dollar spot disease, brown spot disease and leaf spot disease of the bentgrass. The existing drug certificates for this fungicide also include control of various leaf and soil diseases in lawns, commercial bonsai, vegetables, fruit trees, and control of sclerotinia disease occurring in peanuts. The utility of Yiputong as a nematicide is described in EP 1 941 798.
如前所述,本發明組成物還含有一種來自通式(I)及(II)化合物的巨環內酯(macrolide)物質。通式(I)及(II)的巨環內酯(macrolide)化合物於本領域為人所知。巨環內酯(macrolide)為米爾貝霉素(milbemycin)及阿維菌素(avermectin)的物質類別,於US 4,310,519、US 5,077,298、DE 2 717 040及US 4,427,663等有所記載。巨環內酯(macrolide)根據本發明亦可理解為此等物質的衍生物,如米爾貝肟、莫西菌素(moxidectin)、伊維菌素、阿巴汀、因滅汀(emamectin)、 多拉菌素(doramectin),以及通式(I)的賜諾殺(spinosyns)。 As stated previously, the compositions of the present invention also comprise a macrolide material derived from the compounds of formula (I) and (II). Macrolide compounds of the formulae (I) and (II) are known in the art. Macrolides are a class of substances of milbemycin and avermectin, which are described in US 4,310,519, US 5,077,298, DE 2 717 040 and US 4,427,663. Macrolides According to the invention, derivatives of such substances, such as milbemycin, moxidectin, ivermectin, abatatin, emamectin, Doramectin, and spinosyns of the general formula (I).
通式(I)的化合物中,R1應為氫或低級烷基,含有1至4個碳原子,甲基更為理想。R2應為雜環基,通式(IV)的基團則更為理想:
通式(I)的理想化合物為多殺黴素(spinosad)及賜諾特(spinetoram)。 The ideal compound of formula (I) is spinosad and spinetoram.
通式(II)的化合物中,R12應為含有1至8個碳原子的烷基,含有1至6個碳原子較理想,1至4個碳原子則更理想。烷基可為直鏈或支鏈,直鏈則較佳。烷基理想為甲基、乙基、丙基 及丁基。此外,R12也可為烯基,含有2至10個碳原子,2至8個碳原子較理想,2至4個碳原子則更理想。烯基可為直鏈或支鏈,支鏈則較佳。於一實施例中,建議使用結構為支鏈的C6烯基。再者,R12亦可以苯基代替。 In the compound of the formula (II), R 12 should be an alkyl group having 1 to 8 carbon atoms, preferably 1 to 6 carbon atoms, more preferably 1 to 4 carbon atoms. The alkyl group may be straight or branched, and a straight chain is preferred. The alkyl groups are desirably methyl, ethyl, propyl and butyl. Further, R 12 may also be an alkenyl group having 2 to 10 carbon atoms, preferably 2 to 8 carbon atoms, and more preferably 2 to 4 carbon atoms. The alkenyl group may be a straight chain or a branched chain, and a branched chain is preferred. In one embodiment, it is recommended to use a C 6 alkenyl group that is branched. Further, R 12 may be substituted by a phenyl group.
通式(II)的理想巨環內酯(macrolide)化合物為伊維菌素、阿巴汀、密滅汀、莫西菌素、依普菌素(eprinomectin)、雷皮菌素(lepimectin)、色拉菌素(selamectin)、多拉菌素。 The ideal macrolide compound of the formula (II) is ivermectin, abatatin, metostatin, moxidectin, eprinomectin, lepimectin, Selamectin, doramectin.
通式(I)及(II)巨環內酯(macrolide)化合物會以自由單體形式或鹽的形式運用。巨環內酯(macrolide)化合物的農化兼容鹽例如:無機及有機酸的酸加成鹽,特別是氫氯酸、氫溴酸、硫酸、硝酸、高氯酸、磷酸、甲酸、乙酸、三氟乙酸、草酸、丙二酸、甲苯磺酸或苯甲酸。 The macrolide compounds of the formulae (I) and (II) are used in the form of free monomers or salts. Agrochemically compatible salts of macrolide compounds such as acid addition salts of inorganic and organic acids, especially hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, perchloric acid, phosphoric acid, formic acid, acetic acid, three Fluoroacetic acid, oxalic acid, malonic acid, toluenesulfonic acid or benzoic acid.
阿巴汀是一種建議使用於本發明的組成物的巨環內酯(macrolide)化合物。阿巴汀是阿維菌素B1a及阿維菌素B1b的混合物.並於倫敦英國作物委員會的農藥手冊第十版(1994)第三頁等刊物有所記載。阿巴汀是於市場上有售的化合物。 Abastatin is a macrolide compound suggested for use in the compositions of the present invention. Abatatin is a mixture of avermectin B 1a and avermectin B 1b . It is also recorded in the third edition of the Pesticide Manual of the British Crop Commission in London (1994). Abatatin is a commercially available compound.
因滅汀(emamectin)(4"-De-oxy-4"-epi-N-methylamino avermectin B1b/B1a)是另一種建議使用的巨環內酯(macrolide)化合物,於US 4,874,749有所記載。因滅汀又稱MK-244,載於有機化學期刊第59卷(1994)第7704至7708頁。對農化範疇甚為有用的因滅汀鹽列載於US 5,288,710。 Emamectin (4"-De-oxy-4"-epi-N-methylamino avermectin B 1b /B 1a ) is another proposed macrolide compound and is described in US 4,874,749. . Insecticide, also known as MK-244, is contained in the Journal of Organic Chemistry, Vol. 59 (1994), pp. 7704 to 7708. The statin salt, which is very useful for the agrochemical category, is listed in US 5,288,710.
此外,另一種建議使用的巨環內酯(macrolide)化合物包括:含有賜諾殺及其衍生物的化合物組合;含有天然賜諾殺的化合物組合;及含有天然賜諾殺的衍生物的化合物組合。活性成份應含有賜諾殺A、賜諾殺D、或賜諾殺A及賜諾殺D的混合物。一種特別成分為多殺黴素。多殺黴素記載於英國倫敦英國作物委員會的農藥手冊第十一版(1997)第1272至1273頁。 In addition, another proposed macrolide compound includes: a combination of compounds containing spinosad and its derivatives; a combination of compounds containing natural spinosad; and a combination of compounds containing natural derivatives. . The active ingredient should contain a mixture of sinus A, sinus D, or sinus A and sin. One particular ingredient is doxorubicin. Spinosad is described in the 11th edition of the Pesticide Manual of the British Crop Commission, London, UK (1997), pp. 1272 to 1273.
本發明的建議實施例為一種組成物,含有阿巴汀或多殺黴素,太多是自由單體形式,或因滅汀,大多是鹽的形式,尤其苯甲酸鹽,作為巨環內酯(macrolide)活性成分。 A preferred embodiment of the invention is a composition comprising abatatin or spinosad, too much in the form of a free monomer, or in the form of a salt, mostly in the form of a salt, especially a benzoate, as a macrocycle An active ingredient of macrolide.
此組成物可能含有任何合適份量的依普同。本發明的一些實施例中,含按重量計1%至99%的依普同,其中30%至90%較理想,50%至80%更為理想。 This composition may contain any suitable amount of Yiputong. In some embodiments of the invention, from 1% to 99% by weight, more preferably from 30% to 90%, more preferably from 50% to 80%.
組成物可能含有任何合適份量的通式(I)及(II)的巨環內酯(macrolide)化合物。本發明的一些實施例中,含有按重量計1%至50%來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物,其中5%至40%較理想,10%至30%更為理想。 The composition may contain any suitable amount of macrolide compounds of formula (I) and (II). In some embodiments of the invention, from 1% to 50% by weight of macrolide compounds from the compounds of formula (I) and (II), of which 5% to 40% are preferred, 10% to 30% is more ideal.
組成物可能含有一種來自通式(I)及(II)化合物的單一巨環內酯(macrolide)化合物。另一方面,組成物可能含有兩種或以上通式(I)及(II)的巨環內酯(macrolide)化合物的混合物。 The composition may contain a single macrolide compound from the compounds of formula (I) and (II). On the other hand, the composition may contain a mixture of two or more macrolide compounds of the formulae (I) and (II).
依普同及來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物之重量比於1:100至100:1之間,1:50至50:1較為理想。 The weight ratio of the macrolide compound from the compounds of the general formulae (I) and (II) is between 1:100 and 100:1, and preferably 1:50 to 50:1.
本發明的農用化學品組成物可能更含有一種或多種農業可接受助劑。組成物使用的助劑及其份量將因應配方的類型及/或最終使用者使用配方方法而定。合適助劑為一般配方助劑或成分,如溶劑、表面活性劑、穩定劑、抗泡劑、防凍劑、防腐劑、抗氧化劑、色素、增稠劑及惰性填充劑。有關助劑於本領域廣為人知及於市面上有售。本領域的技術人士熟悉此等助劑於本發明組成物配方的用途。 The agrochemical compositions of the present invention may further comprise one or more agriculturally acceptable adjuvants. The amount of auxiliaries used in the composition and the amount thereof will depend on the type of formulation and/or the formulation method used by the end user. Suitable auxiliaries are general formulation auxiliaries or ingredients such as solvents, surfactants, stabilizers, antifoaming agents, antifreeze agents, preservatives, antioxidants, pigments, thickeners and inert fillers. The auxiliaries are well known in the art and are commercially available. Those skilled in the art are familiar with the use of such adjuvants in the formulation of the compositions of the present invention.
組成物可能含有一種或多種溶劑。溶劑分別為有機或無機。合適溶劑來自一般溶劑,能完全溶解所使用的農化活性物質。合適溶劑於本領域廣為人知及於市面上有售。合適溶劑例子包括水;芳香烴溶劑如二甲苯(例如SolvessoTM於市面有售的溶劑產品);礦物油;動物油;植物油;酒精,如甲醇、丁醇、 戊醇及苯甲醇;酮,如環己酮及γ-丁內酯;吡咯酮,如NMP及NOP;醋酸鹽,如二乙酸酯;二醇類;脂肪酸二甲基酰胺;脂肪酸;及脂肪酸脂。 The composition may contain one or more solvents. The solvents are organic or inorganic, respectively. A suitable solvent is derived from a general solvent to completely dissolve the agrochemical active substance used. Suitable solvents are well known in the art and are commercially available. Examples of suitable solvents include water; aromatic hydrocarbon solvents such as xylene (e.g., Solvesso (TM) is a commercially available solvent product); mineral oil; animal oil; vegetable oil; alcohols such as methanol, butanol, pentanol and benzyl alcohol; Hexanone and γ-butyrolactone; pyrrolidone such as NMP and NOP; acetate such as diacetate; glycol; fatty acid dimethylamide; fatty acid;
組成物更可含有一種或多種表面活性劑。合適表面活性劑於本領域廣為人知,包括但不限於鹼金屬、鹼土金屬;及木質磺酸、萘磺酸、酚磺酸(phenolsulfonic acid)、二丁萘磺酸、烷基芳基磺酸鹽、烷基硫酸鹽、烷基磺酸鹽、芳基磺酸鹽、脂肪醇硫酸鹽、脂肪酸及硫化脂肪酸二醇脂的銨鹽。此外還包括磺化萘及萘衍生物的濃縮物(含甲醛)、萘濃縮物或萘磺酸濃縮物,其中含酚、辛苯酚、壬苯酚、烷基苯基聚乙二醇醚、三丁基苯基聚乙二醇醚(tributylphenyl polyglycol ether)、三硬脂苯基聚乙二醇醚(tristearylphenyl polyglycol ether)、烷基芳基聚醚醇、醇及脂肪醇/環氧乙烷濃縮物、乙氧化蓖麻油、聚氧乙烯烷基醚、乙氧化聚氧丙烯、月桂醇聚二醇醚縮醛、山梨醇酯、木質素亞硫酸鹽廢液,以及甲基纖維素及氧化乙烯/氧化丙烯塊狀共聚物。合適表面活性劑於市面上有售。 The composition may further comprise one or more surfactants. Suitable surfactants are well known in the art, including, but not limited to, alkali metals, alkaline earth metals; and lignosulfonic acid, naphthalenesulfonic acid, phenolsulfonic acid, dibutylnaphthalenesulfonic acid, alkylarylsulfonates, Alkyl sulfates, alkyl sulfonates, aryl sulfonates, fatty alcohol sulfates, fatty acids and ammonium salts of sulfurized fatty acid glycol esters. Also included are concentrates (including formaldehyde), naphthalene concentrates or naphthalenesulfonic acid concentrates of sulfonated naphthalene and naphthalene derivatives, which contain phenol, octylphenol, decylphenol, alkylphenyl polyglycol ether, and tributylene. Triphenyl phenyl polyglycol ether, tristearylphenyl polyglycol ether, alkyl aryl polyether alcohol, alcohol and fatty alcohol/ethylene oxide concentrate, Ethylene oxide castor oil, polyoxyethylene alkyl ether, ethoxylated polyoxypropylene, lauryl polyglycol ether acetal, sorbitol ester, lignin sulfite waste liquid, and methyl cellulose and ethylene oxide / propylene oxide Block copolymer. Suitable surfactants are commercially available.
組成物可再含有一種或多種聚合物穩定劑。合適聚合物穩定劑可於本發明使用,包括但不限於聚丙烯、聚異丁烯、聚異戊二烯、單烯烴及二烯烴的共聚物、聚丙烯酸酯、聚苯乙烯、聚醋酸乙烯酯、聚胺酯或聚醯胺。合適穩定劑於本領域廣為人知及於市面上有售。 The composition may further comprise one or more polymeric stabilizers. Suitable polymeric stabilizers can be used in the present invention, including but not limited to polypropylene, polyisobutylene, polyisoprene, copolymers of monoolefins and diolefins, polyacrylates, polystyrenes, polyvinyl acetates, polyurethanes Or polyamine. Suitable stabilizers are well known in the art and are commercially available.
組成物可包括抗泡劑。合適抗泡劑包括一般用於農用化學品組成物的消泡物質,本領域技術人員將會熟知有關物質。合適抗泡劑於本領域廣為人知及於市面上有售。其中,理想抗泡劑為聚二甲基矽氧烷及全氟烷基磷酸(perfluroalkylphosphonic acid)的混合物,如聚矽氧抗泡劑(例如GE或康普頓(Compton)市面有售的抗泡劑)。 The composition may include an antifoaming agent. Suitable antifoaming agents include antifoaming materials which are generally used in agrochemical compositions, and those skilled in the art will be familiar with the relevant materials. Suitable antifoaming agents are well known in the art and are commercially available. Among them, the ideal antifoaming agent is a mixture of polydimethyl siloxane and perfluroalkylphosphonic acid, such as polyoxyn antifoam (such as GE or Compton). Agent).
組成物可能含有一種或多種防腐劑。合適防腐劑包括一般 用於農用化學品組成物的防腐物質,以及也於本領域廣為人知,可能予以提述的合適例子包括Bayer AG有售的Preventol®及Proxel®。 The composition may contain one or more preservatives. Suitable preservatives include general Preservatives for agrochemical compositions, as well as well known in the art, suitable examples that may be referred to include Preventol® and Proxel® available from Bayer AG.
再者,組成物可能包括一種或多種抗氧化劑。合適抗氧化劑為一般用於農用化學品組成物的抗氧化物質,且於本領域廣為人知,尤其丁基羥基甲苯。 Further, the composition may include one or more antioxidants. Suitable antioxidants are the antioxidants commonly used in agrochemical compositions and are well known in the art, especially butylhydroxytoluene.
組成物可再包括一種或多種固體黏著物。有關黏著物於本領域廣為人知及於市面有售,包括有機黏著物,其中包括膠黏劑(如經取代纖維素的纖維素);天然及合成共聚物的粉劑、粒劑、或晶格;及無機黏著物如石膏、石英及水泥。 The composition may further comprise one or more solid binders. Adhesives are well known in the art and are commercially available, including organic adhesives, including adhesives (such as cellulose substituted cellulose); powders, granules, or crystal lattices of natural and synthetic copolymers; Inorganic adhesives such as gypsum, quartz and cement.
組成物更可含有一種或多種惰性填充劑。有關惰性填充劑於本領域廣為人知及於市面有售。合適填充劑包括天然地面礦物,如高嶺土、礬土、滑石、白堊、石英、凹凸棒土、蒙脫石、及矽藻土或合成地面礦物如高分散矽酸、氧化鋁、矽酸鹽及磷酸鈣及磷酸氫鈣。合適惰性填充劑顆粒包括壓碎及分餾天然礦物,如方解石、大理石、浮石、海泡石、及白雲石、或無機或有機地面物質合成顆粒以及有機物質顆粒如木屑、椰殼、玉米穗軸及煙草莖。 The composition may further comprise one or more inert fillers. Inert fillers are well known in the art and are commercially available. Suitable fillers include natural ground minerals such as kaolin, alumina, talc, chalk, quartz, attapulgite, montmorillonite, and diatomaceous earth or synthetic ground minerals such as highly dispersed tannins, alumina, citrate and phosphoric acid. Calcium and calcium hydrogen phosphate. Suitable inert filler particles include crushed and fractionated natural minerals such as calcite, marble, pumice, sepiolite, and dolomite, or synthetic particles of inorganic or organic ground materials, and organic material particles such as wood chips, coconut shells, corn cobs, and Tobacco stems.
組成物更可含有一種或多種增稠劑。合適增稠劑包括一般用於農用化學品組成物的增稠物質。合適增稠劑例子包括膠土,如黃原膠、聚乙烯醇(PVOH)、纖維素及其衍生物、水矽酸鹽黏土、矽酸鎂鋁或其混合物。有關增稠劑也於本領域廣為人知及於市面有售。 The composition may further contain one or more thickeners. Suitable thickeners include thickening materials commonly used in agrochemical compositions. Examples of suitable thickeners include clays such as xanthan gum, polyvinyl alcohol (PVOH), cellulose and its derivatives, hydroxamate clay, magnesium aluminum silicate or mixtures thereof. Thickeners are also well known in the art and are commercially available.
本發明的一些實施例中,農用化學品組成物可以純組成物形式使用或如上所述,建議可連同最少一種助劑使用。 In some embodiments of the invention, the agrochemical composition may be used in the form of a pure composition or as described above, and may be used in conjunction with at least one adjuvant.
本發明組成物亦可含有其他活性成分以達到指定效果,例如殺菌劑、殺真菌劑、殺蟲劑、殺線蟲劑、除螺劑或除草劑。上述應用所需的合適化合物於本領域廣為人知及於市面上有 售。 The compositions of the present invention may also contain other active ingredients to achieve a specified effect, such as bactericides, fungicides, insecticides, nematicides, de-gelling agents or herbicides. Suitable compounds for the above applications are well known in the art and are commercially available. Sold.
本發明農用化學品組成物可按其用途以不同方法調製。合適製劑技術於本領域廣為人知,包括水分散粉劑、粉劑、糊劑、水分散性顆粒、水溶液、可乳化濃縮物、乳液、水懸劑、懸乳劑、噴霧劑、或微膠囊懸浮液。建議農用化學品組成物可調製成水分散顆粒、可乳化濃縮物、水懸劑、懸乳劑、或微膠囊懸浮液。 The agrochemical composition of the present invention can be prepared in various ways depending on its use. Suitable formulation techniques are well known in the art and include aqueous dispersion powders, powders, pastes, water-dispersible granules, aqueous solutions, emulsifiable concentrates, emulsions, aqueous suspensions, suspoemulsions, sprays, or microcapsule suspensions. It is recommended that the agrochemical composition be made into water-dispersible granules, emulsifiable concentrates, aqueous suspensions, suspoemulsions, or microcapsule suspensions.
本發明使用的製劑類型例子如下: Examples of the types of preparations used in the present invention are as follows:
把依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物溶於水溶性溶劑,可加入一種或多種濕潤劑及/或其他助劑。加水稀釋後,活性化合物隨之溶化。 One or more wetting agents and/or other auxiliaries may be added to the water-soluble solvent by dissolving at least one macrolide compound derived from the compounds of the general formulae (I) and (II). After dilution with water, the active compound is dissolved.
把依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物溶於不混水溶劑,建議加入一種或多種非陰離子乳化劑及陰離子乳化劑。以如攪拌等方法攪勻混合物,製成均勻的製劑。加水稀釋後,產生穩定乳液。 It is recommended to add one or more non-anionic emulsifiers and anionic emulsifiers to the non-aqueous solvent in which the macrolide compound of the formula (I) and (II) is dissolved in a solvent. The mixture is stirred by a method such as stirring to prepare a uniform preparation. After dilution with water, a stable emulsion is produced.
把依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物溶於一種或多種合適的不混水溶劑,建議加入一種或多種非陰離子乳化劑及陰離子乳化劑。所產生混合物使用合適工具如乳化機器加入水中,以形成均勻乳液。再加水稀釋後,產生穩定乳液。 It is recommended to add one or more non-anionic emulsifiers and anions to one or more suitable non-aqueous solvents in a solution of at least one macrolide from the compounds of formula (I) and (II). Emulsifier. The resulting mixture is added to water using a suitable tool such as an emulsification machine to form a homogeneous emulsion. After dilution with water, a stable emulsion is produced.
於攪拌球磨機中,把依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物磨成粉末,建議加入一種或多種分散劑及濕潤劑,以及水或溶劑,產生細碎活性化合物懸浮液。加水稀釋後,產生穩定的活性化合物懸浮液。 In a stirred ball mill, a macrolide compound of the formula (I) and (II) is pulverized into a powder, and it is recommended to add one or more dispersing agents and wetting agents, and water or The solvent produces a finely divided suspension of the active compound. Upon dilution with water, a stable suspension of the active compound is produced.
細磨依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物,建議加入一種或多種分散劑及濕潤劑,並使用合適技術如擠壓、於噴霧塔瀝乾、或經流體化床處理,製成水分散性或水溶性顆粒。加水稀釋後,產生穩定分散液或活性化合物溶液。 Finely pulverizing and at least one macrolide compound derived from the compounds of the formulae (I) and (II), it is recommended to add one or more dispersing agents and wetting agents, and using suitable techniques such as extrusion, spraying The column is drained or treated with a fluidized bed to form water-dispersible or water-soluble particles. After dilution with water, a stable dispersion or active compound solution is produced.
在合適儀器如動靜磨機磨碎依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物,建議加入一種或多種分散劑、濕潤劑及矽膠。加水稀釋後,產生穩定分散液或活性化合物溶液。 It is advisable to add one or more dispersing agents, wetting agents and silicones in a suitable apparatus such as a static and dynamic mill to grind E. coli and at least one macrolide compound from the compounds of the formulae (I) and (II). After dilution with water, a stable dispersion or active compound solution is produced.
在合適儀器加入按重量計不多於99.5份載體,且細磨依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物。然後,使用合適技術如擠壓、噴乾、或使用流體化床製成顆粒。 In a suitable apparatus, no more than 99.5 parts by weight of the carrier are added, and a macrolide compound derived from the compounds of the formulae (I) and (II) is finely ground and at least one. The granules are then formed using suitable techniques such as extrusion, spray drying, or using a fluidized bed.
另一方面,本發明提供使用前述組成物控制某一地點的害蟲方法,尤其用作殺線蟲的方法。 In another aspect, the invention provides a method of controlling pests at a location using the foregoing compositions, particularly as a method of nematicidal.
此外,另一方面,本發明提供防治某一地點的害蟲方法,尤其線蟲,包括於地點應用上述組成物。 Moreover, in another aspect, the invention provides a method of controlling pests at a location, particularly a nematode, comprising applying the above composition at a location.
應用方面,本發明組成物可用於目標植物或有關植物的某個或多個部分(如葉部或種子)或用於植物地點。 In terms of application, the compositions of the invention can be used in one or more parts of a target plant or related plant (such as leaves or seeds) or on a plant site.
另一方面,本發明提供防治於某一地點的線蟲及其他植物害蟲及病原體的方法,包括於地點使用依普同及最少一種來自通式(I)及(II)化合物的巨環內酯(macrolide)化合物。上述活性化合物可於地點分開使用(例如同時或連續使用)。此外,活性化合物可一併使用,建議以上述組成物的方式使用。 In another aspect, the invention provides a method of controlling nematodes and other plant pests and pathogens at a locus comprising the use of ipproxil and at least one macrolide from the compounds of formula (I) and (II) Macrolide) compound. The above active compounds can be used separately at the site (for example, simultaneously or continuously). Further, the active compounds may be used in combination, and it is recommended to use them in the form of the above composition.
其中,本發明農用化學品組成物及方法可用於控制線蟲及 其他植物害蟲及病原體,如:‧線蟲來自的類別包括根瘤線蟲、胞囊線蟲、穿孔線蟲、劍線蟲、矛線蟲、釘線蟲、腎形線蟲、腐線蟲、環形線蟲、螺旋線蟲、刺線蟲、短粗(stubby)線蟲、矮化線蟲、球莖線蟲、種瘤及葉芽線蟲;‧微細毛剌線蟲(Paratrichodorus minor)、長針線蟲屬(Longidorus spp.)、偽强壯螺旋線蟲(Helicotylenchus pseudorobustus)、帽形紐帶線蟲(Hoplolaimus galeatus)、矛狀線蟲(H.columbus)、墊刃形紐帶線蟲(H.tylenchiformis)、毛剌線蟲(Trichodorus proximus)、標準劍線蟲(Xiphinema index)、美洲劍線蟲(X.americanum)、莖線蟲(Ditylenchus dipsaci)、馬鈴薯莖線蟲(D.destructor)、假根瘤線蟲(Nacobbus aberrans)、短環長針線蟲(Longidorus breviannulatus)、非洲長針線蟲(L.africanus)、環腐線蟲(Mesocriconema xenoplax)、水稻葉芽線蟲(Aphelenchoides besseyi)、草莓葉芽線蟲(A.fragariae)、墊刃形紐帶線蟲(Zygotylenchus guevarai)、長尾刺線蟲(Belonolaimus longicaudatus)、細小剌線蟲(B.gracilis)、小麥粒線蟲(Anguina tritici)、腎形線蟲屬(Rotylenchulus spp.)、小麥腫癭線蟲屬(Subanguina spp.)、小環紋線蟲屬(Criconemella spp.)、輪線蟲屬(Criconemoides spp.)、錐線蟲屬(Dolichodorus spp.)、半輪線蟲屬(Hemicriconemoides spp.)、鞘線蟲屬(Hemicycliophora spp.)、潛根線蟲屬(Hirschmaniella spp.)、根結線蟲屬(Hypsoperine spp.)、大節片線蟲屬(Macroposthonia spp.)、矮化線蟲屬(Melinius spp.)、斑皮線蟲屬(Punctodera spp.)、五溝線蟲屬(Quinisulcius spp.)、盾狀線蟲屬(Scutellonema spp.)、及矮化線蟲屬(Tylenchorhynchus spp.); ‧來自腫癭線蟲屬(Anguina spp.);葉芽線蟲屬(Aphelenchoides spp.);莖線蟲屬(Ditylenchus spp.);‧來自黃金線蟲屬(Globodera spp.),例如馬鈴薯黃金線蟲(G.rostochiensis),及馬鈴薯包囊線蟲(G.pallida);長針線蟲屬(Longidorus spp.);‧來自根瘤線蟲屬(Meloidogyne spp.),例如南方根瘤線蟲(Meloidogyne incognita)及爪哇根瘤線蟲(Meloidogyne javanica);‧來自短體線蟲屬(Pratylenchus),例如螺旋短體線蟲(P.neglectans)、斯克裏布納短體線蟲(P.scribneri)、索式短體線蟲(P.thornei)、短小短體線蟲(P.brachyurus)、咖啡短體線蟲(P.coffeae)、玉米短體線蟲(P.zeae),和穿剌短體線蟲(P.penetrans);‧來自穿孔線蟲屬(Radopholus spp.),例如香蕉穿孔線蟲(Radopholus similis)、柑橘穿孔線蟲(R.citrophilus);‧來自針線蟲屬(Trichodorus spp.);穿刺線蟲(Tylenchulus),例如半穿刺線蟲(Tylenchulus semipenetrans);及劍線蟲屬(Xiphinema spp.);‧來自胞囊線蟲屬(Heterodera spp.),例如甜菜胞囊線蟲(H.schachtii)、禾穀胞囊線蟲(H.avenae)、大豆胞囊線蟲(H.glycines)、胡蘿蔔胞囊線蟲(H.`carotae)、豌豆胞囊線蟲(H.goettingiana)、玉米胞囊線蟲(H.zeae)及三葉草胞囊線蟲(H.trifolii);及‧來自根瘤線蟲屬(Meloidogyne spp.),例如南方根瘤線蟲(M.incognita)、爪哇根瘤線蟲(M.javanica)、北方根瘤線蟲(M.hapla)、花生根瘤線蟲(M.arenaria)、哥倫比亞根瘤線蟲(M.chitwoodi)、禾本科根瘤線蟲(M.graminis)、瑪雅古根瘤線 蟲(M.mayaguensis)、法拉克斯根瘤線蟲(M.fallax)、納西根瘤線蟲(M.naasi)。 Among them, the agrochemical composition and method of the present invention can be used for controlling nematodes and other plant pests and pathogens, such as: ‧ nematodes from categories including nodule nematodes, cyst nematodes, perforating nematodes, sword nematodes, spear nematodes, nail nematodes, kidneys Nematodes, rot nematodes, circular nematodes, spiral nematodes, thorn nematodes, stubby worms, dwarf nematodes, bulbous nematodes, tumors and leaf bud nematodes; ‧ Paratrichodorus minor, Longidarus Spp.), Helicotylenchus pseudorobustus, Hoplolaimus galeatus, H. columbus, H. tylenchiformis, Trichodorus proximus, The standard Xiphinema index, X. americanum, Ditylenchus dipsaci, D. destructor, Nacobbus aberrans, Longidorus breviannulatus, L. africanus, Mesocriconema xenoplax, Aphelenchoides besseyi, grass A. fragariae, Zygotylenchus guevarai, Belonolaimus longicaudatus, B. gracilis, Anguina tritici, Rotylenchulus spp .), Subanguina spp., Criconemella spp., Criconemoides spp., Dolichodorus spp., Hemicriconemoides spp .), Hemicycliophora spp., Hirschmaniella spp., Hypsoperine spp., Macroposthonia spp., Melinius spp .), Punctodera spp., Quinisulcius spp., Scutellonema spp., and Tylenchorhynchus spp.; ‧ from the genus Nematode (Anguina spp.); Aphelenchoides spp.; Ditylenchus spp.; ‧ from Globodera spp., such as G. rostochiensis, and potato cyst nematode (G.pallida) Longidorus spp.; ‧ from Meloidogyne spp., such as Meloidogyne incognita and Meloidogyne javanica; ‧ from the genus Pratylenchus, such as a short spiral P. neglectans, P. scribneri, P. thornei, P. brachyurus, P. coffeae ), P. zeae, and P. penetrans; ‧ from Radopholus spp., such as Radopholus similis, citrus perforating nematodes (R. Citrophilus); from Trichodorus spp.; Tylenchulus, such as Tylenchulus semipenetrans; and Xiphinema spp.; ‧ from Heterodera spp. , for example, sugar beet cyst nematode (H.schachtii), cereal cyst nematode (H.avenae), soybean cyst nematode (H.glycines), carrot cyst nematode (H. `carotae), pea cyst nematodes (H .goettingiana), corn cyst nematode (H.zeae) and H. trifolii; and ‧ from Meloidogyne spp., such as M. incognita, M. javanica, M. hapla , M. arenaria, M. chitwoodi, M. graminis, M. mayaensis, M. fallax, Neisseria nematode (M. naasi).
‧來自鱗翅目(Lepidoptera),例如長翅卷蛾屬(Acleris spp.)、褐帶卷蛾屬(Adoxophyes spp.),尤其棉褐帶卷蛾(Adoxophyes reticulana);透翅蛾屬(Aegeria spp.)、夜蛾屬(Agrotis spp.),尤其小劍切根蟲(Agrotis spinifera);棉葉波紋夜蛾(Alabama argillaceae)、澱粉樣屬(Amylois spp.)、黎豆夜蛾(Anticarsia gemmatalis)、黃卷蛾屬(Archips spp.)、帶卷蛾屬(Argyrotaenia spp.)、紋夜蛾屬(Autographa spp.)、玉米蛀莖褐夜蛾(Busseola fusca)、乾果斑螟(Cadra cautella)、桃小食心蟲(Carposina nipponensis)、二化螟屬(Chilo spp.)、色卷蛾屬(Choristoneura spp.)、葡萄果蠹蛾(Clysia ambiguella)、縱卷葉野螟屬(Cnaphalocrocis spp.)、卷蛾屬(Cnephasia spp.)、細卷蛾屬(Cochylisspp.)、鞘蛾屬(Coleophora spp.)、大菜螟(Crocidolomia binotalis)、蘋果異形小卷蛾(Cryptophlebia leucotreta)、小卷蛾屬(Cydia spp.),尤其蘋果蠹蛾(Cydia pomonella);灰杆草螟屬(Diatraea spp.)、展葉松夜蛾(Diparopsis castanea)、實蛾屬(Earias spp.)、乾果斑螟屬(Ephestia spp.)、尤其地中海粉螟(E.Khüniella);白小卷蛾屬(Eucosma spp.)、葡萄與蘋果捲葉蛾(Eupoecilia ambiguella)、茶黃毒蛾屬(Euproctis spp.)、切根蟲屬(Euxoa spp.)、小食心蟲屬(Grapholita spp.)、雲霧廣翅小卷蛾(Hedya nubiferana)、夜蛾屬(Heliothis spp.)、尤其菸草青蟲(H.virescens)and玉米穗蟲(H.zea);菜心野螟(Hellula undalis)、美國白蛾(Hyphantria cunea)、茄莖麥蛾(Keiferia lycopersicella)、旋紋潛蛾(Leucoptera scitella)、細蛾屬(Lithocollethis spp.)、小捲蛾屬(Lobesia spp.)、毒蛾屬(Lymantria spp.)、潛蛾 屬(Lyonetia spp.)、天幕毛蟲屬(Malacosoma spp.)、甘藍夜蛾(Mamestra brassicae)、煙草天蛾(Manduca sexta)、尺蠖蛾屬(Operophtera spp.)、玉米螟(Ostrinia Nubilalis)、超小卷蛾屬(Pammene spp.)、褐卷蛾屬(Pandemis spp.)、小眼夜蛾(Panolis flammea)、紅鈴麥蛾屬(Pectinophora spp.)、馬鈴薯麥蛾(Phthorimaea operculella)、小菜粉蝶日本亞種(Pieris rapae)、毛連菜屬(Pieris spp.)、菜蛾(Plutella xylostella)、巢蛾屬(Prays spp.)、白螟屬(Scirpophaga spp.)、大螟屬(Sesamia spp.)、長須卷蛾屬(Sparganothis spp.)、海灰翅葉蛾(Spodopteralittoralis)、猛透翅蛾屬(Synanthedon spp.)、帶蛾屬(Thaumetopoea spp.)、卷葉蛾屬(Tortrix spp.)、粉紋夜蛾(Trichoplusia ni)和巢蛾屬(Yponomeuta spp.);‧來自鞘翅目(Coleoptera),例如,金針蟲屬(Agriotes spp.)、花象甲屬(Anthonomus spp.)、甜菜隱食甲(Atomaria linearis)、甜菜莖跳甲(Chaetocnema tibialis)、象甲屬(Cosmopolites spp.)、栗象屬(Curculio spp.)、皮屬(Dermestes spp.)、葉甲屬(Diabrotica spp.)、豆瓢蟲屬(Epilachna spp.)、Eremnus spp.、馬鈴薯葉甲(Leptinotarsa decemlineata)、稻象屬(Lissorhoptrus spp.)、鰓角金龜屬(Melolontha spp.)、Orycaephilus spp.、草莓根象甲屬(Otiorhynchus spp.)、Phlyctinusspp.、弧麗拔屬(Popillia spp.)、跳甲屬(Psylliodes spp.)、穀蠹屬(Rhizopertha spp.)、金龜甲科(Scarabeidae)、米象屬(Sitophilus spp.)、麥蛾屬(Sitotroga spp.)、粉蟲屬(Tenebrio spp.)、擬古穀屬(Tribolium spp.)和皮蠹屬(Trogoderma spp.); ‧來自直翅目(Orthoptera),例如,蠊屬(Blatta spp.)、小蠊屬(Blattella spp.)、螻蛄屬(Gryllotalpa spp.)、馬德拉蜚蠊(Leucophaea maderae)、飛蝗屬(Locusta spp.)、大蠊屬(Periplaneta ssp.)、和蚱蜢屬(Schistocerca spp.);‧來自等翅目(Isoptera),例如,犀白蟻屬(Reticulitemes spp);‧來自嚙蟲目(Psocoptera),例如,書虱屬(Liposcelis spp.);‧來自虱目(Anoplura),例如,血虱屬(Haematopinus spp.)、長顎虱屬(Linognathus spp.)、虱屬(Pediculus spp.)、天疱瘡屬(Pemphigus spp.)和根瘤蚜屬(Phylloxera spp.);‧來自食毛目(Mallophaga),例如Damalinea spp.和嚙毛虱屬(Trichodectes spp.);‧來自纓翅目(Thysanoptera),例如,花薊馬屬(Franklinella spp.)、條薊馬屬(Hercinothrips spp.)、帶薊馬屬(Taeniothrips spp.)、薊馬(Thrips palmi)、煙薊馬(Thrips tabaci)和非洲桔硬薊馬(Scirtothrips aurantii);‧來自异翅亞目(Heteroptera),例如,臭蟲屬(Cimex spp.)、可可瘤盲蝽(Distantiella theobroma)、蛇莓屬(Dysdercus spp.)、Euchistus spp.、扁盾蝽屬(Eurygaster spp.)、稻緣蝽屬(Leptocorisa spp.)、綠蝽屬(Nezara spp.)、網蝽屬(Piesma spp.)、長紅獵蝽屬(Rhodnius spp.)、可可褐盲蝽屬(Sahlbergella singularis)、黑蝽屬(Scotinophara spp.)和錐蝽屬(Triatoma spp.);‧來自同翅目(Homoptera),例如,綿粉虱(Aleurothrixus floccosus)、Aleyrodes brassicae、圓盾蚧屬(Aonidiella spp.)、蚜科(Aphididae)、蚜屬(Aphis spp.)、圓盾蚧屬(Aspidiotus spp.)、團扇薺(Bemisia tabaci)、蠟蚧屬(Ceroplaster spp.)、茶褐圓蚧(Chrysomphalus aonidium)、薔薇軟蚧(Chrysomphalus dictyospermi)、褐軟蚧 (Coccushesperidum)、微葉蟬屬(Empoasca spp.)、蘋果綿蚜(Eriosomalarigerum)、斑葉蟬屬(Erythroneura spp.)、Gascardia spp.、飛虱屬(Laodelphax spp.)、Lacanium comi、牡蠣盾蚧屬(Lepidosaphes spp.)、長管蚜屬(Macrosiphus spp.)、瘤蚜屬(Myzus spp.)、Nehoteftix spp.、飛虱屬(Nilaparvata spp.)、環翅卷蛾屬(Paratoria spp.)、瘦綿蚜屬(Pemphigus spp.)、粉蚧屬(Planococcus spp.)、白蚧屬(Pseudaulacaspis spp.)、粉蚧屬(Pseudococcus spp.)、木虱屬(Psylla spp.)、Pulvinaria aethiopica、圓盾蚧屬(Quadraspidiotus spp.)、縊管蚜屬(Rhopalosiphum spp.)、盔蚧屬(Saissetia spp.)、葉蟬屬(Scaphoideus spp.)、二叉蚜屬(Schizaphis spp.)、芒蚜屬(Sitobion spp.)、溫室粉虱(Trialeurodesvaporariorum)、南非柑橘木蝨(Trioza erytreae)和桔盾蚧(Unaspis citri);‧來自膜翅目(Hymenoptera),例如,葉蟻(Acromyrmex)、切葉蟻屬(Atta spp.)、莖鋸蜂屬(Cephus spp.)、葉蜂屬(Diprion spp.)、鋸節葉蜂科(Diprionidae)、雲杉葉蜂(Gilpinia polytoma)、實蜂屬(Hoplocampa spp.)、黑蟻屬(Lasius spp.)、小黃家蟻(Monomorium pharaonis)、鋸角葉蜂屬(Neodiprion spp)、水蟻屬(Solenopsis spp.)和胡蜂屬(Vespa ssp.);‧來自雙翅目(Diptera),例如,伊蚊屬(Aedes spp.)、高粱芒蚊(Antherigona soccata)、花園毛岐(Bibio hortulanus)、紅頭麗蠅(Calliphora erythrocephala)、蠟實蠅屬(Ceratitis spp.)、金蠅屬(Chrysomyia spp.)、庫蚊屬(Culex spp.)、黃蠅屬(Cuterebra spp.)、大實蠅屬(Dacus spp.)、果蠅(Drosophila melanogaster)、厠蠅屬(Fannia spp.)、胃蠅屬(Gastrophilus spp.)、舌蠅屬(Glossina spp.)、皮蠅屬(Hypoderma spp.)、虱蠅屬(Hyppobosca spp.)、潛葉蠅屬(Liriomysa spp.)、綠蠅屬(Lucilia spp.)、潛蠅屬(Melanagromyza spp.)、舍蠅屬(Musca spp.)、狂蠅屬(Oestrus spp.)、稻癭蚊(Orseolia spp.)、瑞典麥秆蠅(Oscinella frit)、黎泉蠅(Pegomyia hyoscyami)、麥蠅屬(Phorbia spp.)、蘋果實蠅(Rhagoletis pomonella)、潭蠅屬(Sciara spp.)、螯蠅屬(Stomoxys spp.)、虻屬(Tabanus spp.)、Tannia spp.、稻大蚊屬(Tipula spp.);‧來自蚤目(Siphonaptera),例如,角葉蚤(Ceratophyllus spp.)和東方鼠蚤(Xenopsyllacheopis);‧來自嬰尾目(Thysanura),例如,西洋衣魚(Lepisma saccharina)及‧來自蜱蟎目(Acarina),例如,粗脚粉蟎(Acarus siro)、柑橘瘤癭蟎(Aceria sheldoni);針剌銹蟎屬(Aculus spp.),尤其蘋果銹蜱(A.schlechtendali);花蜱屬(Amblyomma spp.)、隱喙蜱屬(Argas spp.)、牛蜱屬(Boophilus spp.)、短須蟎屬(Brevipalpus spp.),尤其加州偽葉蟎(B.californicus)及紅偽葉蟎(B.phoenicis);苜蓿苔蟎(Bryobia praetiosa)、上三節癭蟎屬(Calipitrimerus spp.)、皮蟎屬(Chorioptes spp.)、鶏皮刺蟎(Dermanyssus gallinae)、始葉蟎屬(Eotetranychus spp.),尤其鵝耳櫪始葉蟎(E.carpini)及東方始葉蟎(E.orientalis);癭蟎屬(Eriophyes spp.),尤其葡萄癭蟎;玻眼蜱屬(Hyalomma spp.)、硬蜱屬(Ixodes spp.)、草地小爪蟎(Olygonychus pratensis)、鈍喙蜱屬(Ornithodoros spp.)、全爪蟎屬(Panonychus spp.),尤其蘋果全爪蟎(P.ulmi)及柑橘全爪蟎(P.citri);皺葉刺節蜱屬(Phyllocoptruta spp.),尤其柑桔皺葉刺節蜱(P.oleivora);多食跗綫蟎屬(Polyphagotarsonemus spp.), 尤其側多食跗綫蟎(P.latus);瘙蟎屬(Psoroptes spp.)、扇頭蜱屬(Rhipicephalus spp.)、根蟎屬(Rhizoglyphus spp.)、疥蟎屬(Sarcoptes spp.)、跗綫蟎屬(Tarsonemus spp.)和葉蟎屬(Tetranychus spp.),其中包括二點葉蟎(T.urticae)、朱砂葉蟎(T.cinnabarinus)及神澤氏葉蟎(T.Kanzawai)。 ‧ From Lepidoptera, such as Acleris spp., Adoxophyes spp., especially Adoxophyes reticulana; Aegeria spp. ), Agrotis spp., especially Agrotis spinifera; Alabama argillaceae, Amylois spp., Anticarsia gemmatalis, Archips spp., Argyrotaenia spp., Autographa spp., Busseola fusca, Cadra cautella, peach Carposina nipponensis, Chilo spp., Choristoneura spp., Clysia ambiguella, Cnaphalocrocis spp., Moth Genus (Cnephasia spp.), Cochylisspp., Coleophora spp., Crocidolemia binotalis, Cryptophlebia leucotreta, Cydia spp. ), especially Cydia pomonella; Diatraea spp., Diptera moth (Dipar) Eopsis castanea), Earias spp., Ephestia spp., especially E.Khüniella; Eucosma spp., grape and apple leaf moth (Eupoecilia) Ambiguella), Euproctis spp., Euxoa spp., Grapholita spp., Hedya nubiferana, Heliothis spp. ), especially H. virescens and H. zea; Hellula undalis, Hyphantria cunea, Keiferia lycopersicella, Swirling Moucto (Leucoptera scitella), Lythocollethis spp., Lobesia spp., Lymantria spp., moth Genovia spp., Malacosoma spp., Mamestra brassicae, Manduca sexta, Operophtera spp., Ostrinia Nubilalis, ultra-small Pammene spp., Pandemis spp., Panolis flammea, Pectinophora spp., Phthorimaea operculella, small cabbage butterfly Japan Subspecies (Pieris rapae), Pieris spp., Plutella xylostella, Prays spp., Scirpophaga spp., Sesamia spp. , Sparganothis spp., Spodopteralittoralis, Synanthedon spp., Thaumetopoea spp., Tortrix spp. Trichoplusia ni and Yponomeuta spp.; ‧ from Coleoptera, for example, Agriotes spp., Anthonomus spp., beet eclipse Atomaria linearis, Chaetocnema tibialis, Cosmopolites spp., Curcuma (Curcu) Liop spp.), Dermestes spp., Diabrotica spp., Epilachna spp., Eremnus spp., Leptinotarsa decemlineata, Lysorhoptrus spp .), Melonontha spp., Orycaephilus spp., Otiorhynchus spp., Phlyctinusspp., Popillia spp., Psylliodes spp. Rhizopertha spp., Scarabeidae, Sitophilus spp., Sitotroga spp., Tenebrio spp., Tribolium spp. ) and genus Trogoderma spp. ‧From Orthoptera, for example, Blatta spp., Blattella spp., Gryllotalpa spp., Leucophaea maderae, Locusta Spp.), Periplaneta ssp., and Schistocerca spp.; ‧ from Isoptera, for example, Reticulitemes spp; ‧ from Psocoptera For example, Liposcelis spp.; ‧ from Anoplura, for example, Haematopinus spp., Linognathus spp., Pediculus spp., pemphigus Genus (Pemphigus spp.) and Phylloxera spp.; ‧ from Mallophaga, such as Damalina spp. and Trichodectes spp.; ‧ from Thysanoptera, for example, Franklinella spp., Hercinothrips spp., Taeniothrips spp., Thrips palmi, Thrips tabaci, and African orange hard thrips (Scirtothrips aurantii); ‧ from Heteroptera, for example, Cimex spp., cocoa tumor (Distantiella theobroma), Dysdercus spp., Euchistus spp., Eurygaster spp., Leptocorisa spp., Nezara spp., Nettle (Piesma spp.), Rhodnius spp., Sahlbergella singularis, Scotinophara spp., and Triatoma spp.; ‧ from Homoptera (Homoptera), for example, Aleurothrixus floccosus, Aleyrodes brassicae, Aonidiella spp., Aphididae, Aphis spp., Aspidiotus spp. , Bemisia tabaci, Ceroplaster spp., Chrysomphalus aonidium, Chrysomphalus dictyospermi, brown soft palate (Coccushes peridum), Empoasca spp., Eriosomalarigerum, Erythroneura spp., Gascardia spp., Laodelphax spp., Lacanium comi, oyster shield Genus (Lepidosaphes spp.), genus Macrosiphus spp., Myzus spp., Nehoteftix spp., Nilaparvata spp., Paratoria spp. Pemphigus spp., Planococcus spp., Pseudaulaca sps., Pseudococcus spp., Psylla spp., Pulvinaria aethiopica, round Quadraspidiotus spp., Rhopalosiphum spp., Saissetia spp., Scaphoideus spp., Schizaphis spp., genus (Sitobion spp.), Trialeurodes vaporariorum, Trioza erytreae and Unaspis citri; ‧ from Hymenoptera, for example, Acromyrmex, leaf-cutting ants Atta spp., Cephus spp., Diprion spp., Diprionidae Gilpinia polytoma, Hoplocampa spp., Lasius spp., Monomorium pharaonis, Neodiprion spp, water genus Solenopsis spp.) and Vespa ssp.; ‧ from Diptera, for example, Aedes spp., Antherigona soccata, Bibio hortulanus, red head Calliphora erythrocephala, Ceratitis spp., Chrysomyia spp., Culex spp., Cutrebra spp., Daphnia (Dacus) Spp.), Drosophila melanogaster, Fannia spp., Gastrophilus spp., Glossina Spp.), Hypoderma spp., Hyppobosca spp., Liriomysa spp., Lucilia spp., Melanagromyza spp., Musca spp., Oestrus spp., Orseolia spp., Oscinella frit, Pegomyia hyoscyami, Phorbia spp .), Apple fruit fly (Rhagoletis pomonella), Sciara spp., Stomoxys spp., Tabanus spp., Tannia spp., Tipula spp. ; from Siphonaptera, for example, Ceratophyllus spp. and Xenopsyllacheopis; ‧ from the genus Thysanura, for example, Lepisma saccharina and ‧ from the order (Acarina), for example, Acarus siro, Aceria sheldoni, Aculus spp., especially apple rust (A.schlechtendali); Amaranthus (Amblyomma) Spp.), Argas spp., Boophilus spp., Brevipalpus spp., especially California B. californicus and red leafhopper (B.phoenicis); Bryobia praetiosa, Calipitrimerus spp., Chorioptes spp., Dermanyssus gallinae, Eotetranychus spp .), especially E. carpini and E. orientalis; Eriophyes spp., especially vine; Hyalomma spp. Ixodes spp., Olygonychus pratensis, Ornithodoros spp., Panonychus spp., especially P.ulmi and citrus P. citri; Phyllocoptruta spp., especially P. oleivora; Polyphagotarsonemus spp. In particular, P. latus, Psoroptes spp., Rhipicephalus spp., Rhizoglyphus spp., Sarcoptes spp. Tarsonemus spp. and Tetranychus spp., including T. urticae, T. cinnabarinus, and T. Kanzawai. .
本發明的組成物及方法對控制作物內的線蟲特別有效。合適目標作物其中包括穀類,如小麥、大麥、黑麥、燕麥、稻米、玉米、高粱、黍及木薯;甜菜類,如甜菜及飼用甜菜;水果,如梨果、有核水果及無核水果,如蘋果、梨、李子、桃、杏仁、櫻桃及莓類,如草莓、紅莓和黑莓;豆類植物,如豆、扁豆、豌豆及大豆;油料作物,如油菜、芥菜、罌粟、橄欖、向日葵、椰子、蓖麻、可可豆和花生;瓜類,如節瓜、青瓜及瓜果;纖維植物,如棉花、亞麻、大麻和黃麻;柑橘類水果,如橙、檸檬、西柚和橘子;蔬菜,如菠菜、生菜、蘆筍、捲心菜、甘筍、洋蔥、蕃茄、馬鈴薯和辣椒;樟科作物,如牛油果、肉桂、樟腦;以及煙草、堅果、咖啡、茄子、甘蔗、茶、胡椒、藤蔓、蛇麻草、香蕉、天然橡膠作物、桉樹和觀賞作物;其中特別建議採用蕃茄、胡椒、瓜果、咖啡及大豆作物進行處理。 The compositions and methods of the present invention are particularly effective in controlling nematodes in crops. Suitable target crops include cereals such as wheat, barley, rye, oats, rice, corn, sorghum, alfalfa and cassava; beets such as sugar beets and beet; fruits such as pears, nucleated and non-nuclear fruits Such as apples, pears, plums, peaches, almonds, cherries and berries, such as strawberries, cranberries and blackberries; legumes such as beans, lentils, peas and soybeans; oil crops such as canola, mustard, poppies, olives, sunflowers , coconut, ramie, cocoa and peanuts; melons such as melons , cucumbers and melons; fiber plants such as cotton, flax, hemp and jute; citrus fruits such as orange, lemon, grapefruit and orange; Vegetables such as spinach, lettuce, asparagus, cabbage, bamboo shoots, onions, tomatoes, potatoes and peppers; camphor crops such as avocado, cinnamon, camphor; and tobacco, nuts, coffee, eggplant, sugar cane, tea, pepper, vines, Hops, bananas, natural rubber crops, eucalyptus and ornamental crops; special treatments for tomatoes, peppers, melons, coffee and soybeans are recommended.
一般來說,此組成物可予以調製及應用,令依普同及通式(I)及(II)的巨環內酯(macrolide)化合物的農用化學品組成物可按處理地點所需使用任何合適份量。使用份量範圍廣闊,會因應各種因素如土壤成分、應用類別(用於葉面、拌種、播種溝)、目標作物、所防治的線蟲、各自身處的氣候情況、以及按應用類別、應用時間及目標作物而定的其他因素而改變。總括而言,農用化學品組成物用量為每公頃1至約2000克,特別是每公頃10至1000克,理想為每公頃10至500克,更理想為每公頃10至200克。 In general, the composition can be prepared and applied so that the agrochemical composition of the macrolide compound of the general formulae (I) and (II) can be used according to the treatment site. The right amount. The range of use varies widely depending on various factors such as soil composition, application category (for foliar, seed dressing, seeding ditch), target crops, nematodes to be controlled, climate conditions in each area, and application categories and application time. And other factors depending on the target crop. In summary, the agrochemical composition is used in an amount of from 1 to about 2000 grams per hectare, especially from 10 to 1000 grams per hectare, desirably from 10 to 500 grams per hectare, more desirably from 10 to 200 grams per hectare.
根據本發明,依普同及通式(I)及(II)的巨環內酯 (macrolide)活性化合物可以任何上述合適形式使用,以及可同時或於短期內(如於同一天)連續用於需防治的地點。於一個建議實施例中,透過使用本發明的組成物,同時使用依普同與通式(I)及(II)的巨環內酯(macrolide)化合物。依普同及通式(I)及(II)的巨環內酯(macrolide)化合物可不分先後用於植物或地點。各化合物可單次或多次使用。建議各化合物均使用多次,如二至五次,三次則更為理想。 According to the invention, the macrolides of the general formulae (I) and (II) The macrolide active compound can be used in any of the above suitable forms, and can be used continuously or in the short term (e.g., on the same day) for the site to be controlled. In a preferred embodiment, a macrolide compound of the formula (I) and (II) is used simultaneously by using the composition of the present invention. The macrolide compounds of the general formulae (I) and (II) can be used in plants or places, respectively. Each compound can be used one or more times. It is recommended that each compound be used multiple times, such as two to five times, and three times is more desirable.
根據本發明,活性化合物可於任何合適時間使用。本發明的實施例中,活性化合物在種植前、種植時或種植後用於土壤或植物所在地點。可按本領域廣為人知的傳統方法進行有關處理,如滴灌、噴灑及土壤熏蒸。一些實施例中,活性化合物用於植物繁殖物質,如種子(透過種子披衣技術)。此等使用方法及相應使用機器於本領域廣為人知。 According to the invention, the active compound can be used at any suitable time. In an embodiment of the invention, the active compound is applied to the soil or plant location before, during or after planting. The treatment can be carried out according to conventional methods well known in the art, such as drip irrigation, spraying and soil fumigation. In some embodiments, the active compound is used in plant propagation materials, such as seeds (through seed coating techniques). Such methods of use and corresponding use of the machine are well known in the art.
依普同及通式(I)及(II)的巨環內酯(macrolide)化合物可按各自比例使用任何份量。其中,化合物於植物或地點的相對用量如上所述,依普同及通式(I)及(II)的巨環內酯(macrolide)化合物的比例範圍建議為1:100至100:1。 The macrolide compounds of the general formulae (I) and (II) may be used in any proportion in each proportion. Wherein, the relative amount of the compound in the plant or the place is as described above, and the ratio of the ratio of the macrolide compound of the general formula (I) and (II) is recommended to be 1:100 to 100:1.
如果同時使用依普同及通式(I)及(II)的巨環內酯(macrolide)化合物,兩種物質可從不同的製劑來源取得,然後加以混合(即桶混、現成液、噴液、或漿液),及可加入其他殺蟲劑混合;或可從單一製劑混合物取得(即預混、濃縮物、配方化合物(或產品)),及可加入其他殺蟲劑混合。 If both macrolide compounds of the general formulae (I) and (II) are used at the same time, the two substances can be obtained from different preparation sources and then mixed (ie, tank mix, ready-made liquid, spray) Or a slurry), and may be added with other pesticides; or may be obtained from a single formulation mixture (ie, premixed, concentrated, formulated compound (or product)), and may be added with other pesticides.
現以下列例子說明本發明的實施例,僅供說明用途。 The examples of the invention are illustrated by the following examples, for illustrative purposes only.
除本說明或申請專利範圍另有規定外,百分比按重量計算。 Except as otherwise stated in this specification or the scope of the patent application, the percentages are by weight.
水溶性濃縮物製劑以下列組成物調製:
可乳化濃縮物以下列組成物調製:
水分散性粉劑以下列組成物調製:
水分散性顆粒製劑以下列組成物調製:
懸浮液製劑以下列組成物調製:
水溶性濃縮物以下列組成物調製:
水分散性顆粒以下列組成物調製:
種子處理用懸浮劑以下列組成物調製:
水溶性濃縮物以下列組成物調製:
N-甲基吡咯啶酮 合共100克 N-methylpyrrolidone 100 grams total
水分散性顆粒製劑以下列組成物調製:
油水型乳液製劑以下列組成物調製:
懸浮液製劑以下列組成物調製:
於底部為0.25平方米及載有2至3厘米深沙土的膠盒均勻地加入100條南方根瘤線蟲(Meloidogyne incognita)。各處理會重複三次並進行測試。測試使用依普同(Bayer的Rovral®)、阿巴汀(Syngenta的Agador®)、因滅汀苯甲酸鹽(Emamectin Benzoate)(Syngenta的Affirm®)、多殺黴素(陶氏的Success)及上述例1至12各種製劑,並根據24或48小時後的死亡率評估效用。 100 strips of Meloidogyne incognita were evenly added to a plastic box with a bottom of 0.25 square meters and 2 to 3 cm of deep sand. Each treatment was repeated three times and tested. The test used Epson (Bayer's Rovral®), Abatatin (Syngenta's Agador®), Emamectin Benzoate (Syngenta's Affirm®), Doxorubicin (Dow's Success) And the various preparations of the above Examples 1 to 12, and the effects were evaluated based on the mortality after 24 or 48 hours.
結果如下表所載。 The results are presented in the table below.
如上表所見,與市面有售的組成物相比,根據本發明調製的製劑對控制目標害蟲有明顯改善的功效。 As seen in the above table, the formulation prepared according to the present invention has a markedly improved effect on controlling target pests as compared with commercially available compositions.
重複測試1的一般步驟,評估對爪哇根瘤線蟲(Meloidogyne javanica)的殺線蟲活性. Repeat the general procedure of Test 1 to assess the nematicidal activity against Meloidogyne javanica .
結果如下表所載。 The results are presented in the table below.
如上表所見,與市面有售的組成物相比,根據本發明調製的製劑對控制目標害蟲有明顯改善的功效。 As seen in the above table, the formulation prepared according to the present invention has a markedly improved effect on controlling target pests as compared with commercially available compositions.
蕃茄種子於含有商業育苗基質的播種箱內進行播種,並於兩星期後把植物移植到一個十厘米花盆,內載250克(乾重)經蒸汽消毒的砂。每盆放入30000顆爪哇根瘤線蟲(Meloidogyne javanica)卵。使用依普同(Bayer的Rovral®)、阿巴汀(Syngenta的Agador®)、因滅汀苯甲酸鹽(Emamectin Benzoate)(Syngenta的Affirm®)、多殺黴素(陶氏的Success)及上述例1至12各種製劑。花盆以隨機完全區集設計排列,每項處理重複設置六次,且於溫室以室溫及環境光培植。植物按需要每天澆水。處理後一個月,量度植物高度及按根瘤評分0-10(其中0=並無根瘤及10=100%根部表面出現根瘤)評定根瘤情況。 Tomato seeds were sown in a seeding box containing a commercial seedling substrate, and after two weeks the plants were transplanted into a ten centimeter pot containing 250 grams (dry weight) of steam sterilized sand. 30,000 eggs of Meloidogyne javanica were placed in each pot. Use Epson® (Bayer's Rovral®), Abatatin (Syngenta's Agador®), Emamectin Benzoate (Syngenta's Affirm®), Doxorubicin (Dow's Success) and Various formulations of the above Examples 1 to 12. The pots were arranged in a random complete zone design, each treatment was set up six times and planted in the greenhouse at room temperature and ambient light. Plants are watered daily as needed. One month after the treatment, the height of the plants was measured and the nodule was evaluated according to the nodule score of 0-10 (where 0 = no nodule and 10 = 100% root nodules on the root surface).
結果如下表所載。 The results are presented in the table below.
如上表所見,與市面有售的組成物相比,根據本發明調製的製劑對控制目標害蟲有明顯改善的功效。 As seen in the above table, the formulation prepared according to the present invention has a markedly improved effect on controlling target pests as compared with commercially available compositions.
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