WO2022001601A1 - 三氟杀线酯用于防治农业害虫、害螨的用途 - Google Patents

三氟杀线酯用于防治农业害虫、害螨的用途 Download PDF

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WO2022001601A1
WO2022001601A1 PCT/CN2021/099094 CN2021099094W WO2022001601A1 WO 2022001601 A1 WO2022001601 A1 WO 2022001601A1 CN 2021099094 W CN2021099094 W CN 2021099094W WO 2022001601 A1 WO2022001601 A1 WO 2022001601A1
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Prior art keywords
mites
nematicide
acaricide
containing insecticide
test
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PCT/CN2021/099094
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English (en)
French (fr)
Inventor
唐剑峰
迟会伟
吴建挺
徐龙祥
赵恭文
李冬蓉
韩君
王丹丹
袁雪
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山东省联合农药工业有限公司
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Priority to KR1020237003384A priority Critical patent/KR20230029957A/ko
Priority to JP2022578675A priority patent/JP2023531003A/ja
Priority to MX2022016234A priority patent/MX2022016234A/es
Priority to EP21833661.8A priority patent/EP4154713A4/en
Priority to US18/003,579 priority patent/US20230354810A1/en
Priority to AU2021302006A priority patent/AU2021302006B2/en
Priority to BR112022025681A priority patent/BR112022025681A2/pt
Publication of WO2022001601A1 publication Critical patent/WO2022001601A1/zh
Priority to ZA2023/01215A priority patent/ZA202301215B/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/32—Oxygen atoms
    • C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • 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
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
    • A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
    • A01N43/06—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings
    • A01N43/08—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings with oxygen as the ring hetero atom
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01P—BIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P7/00—Arthropodicides
    • A01P7/02—Acaricides
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01P—BIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P7/00—Arthropodicides
    • A01P7/04—Insecticides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Definitions

  • the invention belongs to the field of agricultural insecticides and acaricides, and relates to a product for preventing and controlling agricultural pests and mites, and a preparation method and application thereof, using nematicide as an active ingredient.
  • Triflofenac has activity against a variety of agricultural pest mites, can effectively inhibit the female oviposition of agricultural pest mites, and has outstanding activity on the eggs of pest mites, and Triflufenac has no cross-resistance with existing pesticides, and is an excellent alternative to solve the 3R problem of agricultural pests and mites.
  • Trifloxacin (CAS: 2074661-82-6) has a low toxicity level, is safe to use, and belongs to an environment-friendly compound.
  • the present invention provides an insecticide and acaricide containing nematicide.
  • an effective amount of the insecticide and acaricide to the area where the pests and mites are inhabited, assumed to be inhabited or about to inhabit, mainly by inhibiting the females of the insects and mites. It can reduce the damage of pest mites to crops by laying eggs and inhibiting the hatching of pest mites eggs.
  • the agricultural pest mites are at least one of phytophagous mites, Bemisia tabaci, Mildew mosquitoes, diamondback moths and armyworms (such as corn armyworm).
  • the phytophagous pest mite is at least one selected from the group consisting of Tetranychus cinnabarinus, Tetranychus 2-spotted, Panonychus citrus or Tetranychus hawthorn.
  • the structure of the trifluoromethyl ester is as follows:
  • the present invention also provides an insecticide and acaricide containing nematicide, which comprises nematicide and a solvent.
  • the added amount of trifluoromethyl is 1-80wt%, such as 1-60wt%, such as 1wt%, 2wt%, 5wt% , 8wt%, 10wt%, 12wt%, 15wt%, 20wt%, 25wt%, 30wt%, 35wt%, 40wt%, 45wt%, 50wt%, 55wt%, 60wt%, 70wt% or 80wt%.
  • the nematicide-containing insecticide and acaricide further includes an emulsifier.
  • the added amount of the emulsifier (the mass of the emulsifier in the insecticide and acaricide) is 3-30wt%, such as 3wt%, 5wt%, 8wt%, 10wt%, 12wt%, 15wt%, 20wt%, 25wt%, 28wt% or 30wt%.
  • the nematicide-containing insecticide and acaricide may further include other adjuvants, and the other adjuvants may be thickeners, preservatives, defoaming agents, dispersing agents, stabilizers, moisturizing agents, etc. At least one of a wetting agent, a penetrating agent, an adhesive, etc.; the other adjuvants can make the nematicide-containing insecticide and acaricide to be processed into agriculturally usable products for different use occasions.
  • EC water emulsion, water, wettable powder, microemulsion, suspension, microcapsule suspension or water dispersible granule.
  • the present invention when used as an emulsifiable concentrate for foliar spraying and soil treatment as a product for controlling agricultural pests and mites (that is, an insecticide and acaricide containing nematicide), the formula is:
  • Trifloxacin 1-60wt%
  • Emulsifier 5-20wt%
  • the emulsifier is selected from one or more of Agricultural Milk 100#, TX-10, Agricultural Milk 500#, Agricultural Milk 602#, OP500, OP10, Tween 80 or Agricultural Milk 600#, preferably 5 - At least one of 8 wt% agricultural milk 100#, 5-8 wt% agricultural milk 600#, and 3-8 wt% Tween 80.
  • Production process first add the mixed solvent, then put in the quantitatively weighed trifluoromethyl ester, add the emulsifier and mix well for 0.5 hours to be fully uniform, and then continue to stir in the preparation tank for 0.5 hours. Test the content, pack it in double-barrier plastic bottles, and store in a sealed container.
  • the present invention when used as an aqueous emulsion for foliar spraying and soil treatment as a product for controlling agricultural pests and mites (that is, an insecticide and acaricide containing nematicide), the formula is:
  • Trifloxacin 1-50wt%
  • Emulsifier 12-28wt%
  • the emulsifier is selected from one or more of 7780, 7781T, 4103, Well201, TX-10, agricultural milk 500#, agricultural milk 602# or WellM30, etc., preferably the emulsifier is 5-15wt% of 7780 and 3-12 wt% of 7781T.
  • the solvent is an aromatic hydrocarbon solvent or cyclohexanone or the like.
  • Production process firstly add solvent, then put in quantitatively weighed trifluorodimethoxide, add emulsifier and mix well for 0.5 hours to be fully uniform, and then continue to stir in the preparation tank for 0.5 hours. The mixture was slowly added to water and homogenized. Test the content, pack it in double-barrier plastic bottles in glass bottles or aluminum bottles with inner barrier coating, and store them in a sealed container.
  • the present invention when used as a product for controlling agricultural pests and mites (that is, an insecticide and acaricide containing nematicide) for foliar spraying and soil treatment, the formula is:
  • Trifloxacin 1-80wt%
  • Emulsifier 12-28wt%
  • the emulsifier is betaine.
  • Production process first put in the quantitatively weighed trifluoromethyl ester, add emulsifier, then add water and mix well for 0.5 hours to be fully uniform, and then continue to stir in the preparation tank for 0.5 hours. Test the content, pack it in double-barrier plastic bottles in glass bottles or aluminum bottles with inner barrier coating, and store them in a sealed container.
  • the present invention when used as a suspending agent for foliar spraying and soil treatment as a product for controlling agricultural pests and mites (that is, an insecticide and acaricide containing nematicide), the formula is:
  • Trifloxacin 1-80wt%
  • Emulsifier 1-20wt%
  • the emulsifier is tristyryl fen polyoxyethylene ether phosphate triethanolammonium salt, lignosulfonate or naphthalene sulfonate;
  • the thickener is xanthan gum, magnesium aluminum silicate or gelatin ;
  • the preservative is sodium benzoate or benzoic acid;
  • the defoaming agent is selected from organosilicon additives, and the solvent is selected from water, solvent oil, methyl oleate, turpentine oil or propylene carbonate.
  • Production process firstly, emulsifier, defoamer and water are mixed and homogenized, then put in quantitatively weighed trifluoromethyl ester and solvent, and then homogenized and sanded. After passing the test, add preservatives and thickeners and then homogenize, test the content, and then pack them into double-barrier plastic bottles in glass bottles or aluminum bottles with internal barrier layers, and seal them for storage.
  • Trifloxacin 1-80wt%
  • Emulsifier 12-28wt%
  • the emulsifier is tristyryl fen polyoxyethylene ether phosphate triethanolammonium salt or fatty acid polyoxyethylene ether;
  • the solvent is selected from water, solvent oil, methyl oleate, turpentine oil, propylene carbonate , cyclohexanone or decylamide.
  • Production process firstly add solvent, then put in quantitatively weighed trifluorodimethoxide, add emulsifier and mix well for 0.5 hours to be fully uniform, and then continue to stir in the preparation tank for 0.5 hours. Continue stirring with water in the mixing tank.
  • the present invention also provides a method for preventing and controlling agricultural pests and mites, the method comprising the steps of:
  • the above-mentioned nematicide-containing insecticide and acaricide is applied by foliar spraying or soil treatment to the area where the pest mites inhabit, are supposed to inhabit, or are about to inhabit the insect infestation mites.
  • the above-mentioned nematicide-containing insecticide and acaricide is applied by foliar spraying or soil treatment to the area where the eggs of pest mites inhabit, are supposed to inhabit, or are about to inhabit.
  • Trifluoromethyl ester can be formulated into agriculturally acceptable emulsifiable concentrate, water emulsion, water preparation, wettable powder, microemulsion, suspension, microcapsule suspension or water dispersible granule, wherein trifluoromethyl ester is in the dosage form The content of 1%-80%.
  • the trifluoromethyl ester has outstanding control effect on agricultural pests and mites, and the trifluoromethyl ester is a new compound and has no cross-resistance with existing products.
  • Egg-laying inhibitory activity assay test The original medicinal acetone was prepared into a mother liquor with a mass concentration of 1 wt % for later use, and diluted with deionized water containing 0.1 wt % of Tween 80 to a series concentration of the test.
  • Fresh cowpea seedling leaves were selected and cut into circular leaf discs with a diameter of about 5.0 cm, which were placed in a plastic petri dish covered with filter paper and absorbent cotton. Apply 5 and 10 mg/L treatment agents on the back of the leaves with cotton swabs, and use an aqueous solution with the same solvent ratio as a control agent.
  • Determination test of mite egg hatching inhibitory activity using leaf soaking method to carry out the test, the original medicinal acetone was prepared into a mother liquor with a mass concentration of 1 wt % for use, and diluted with deionized water containing 0.1 wt % Tween 80 to a series of test concentrations. Pour 1.2% agar water into a petri dish with a diameter of 9 cm to cool it for later use; select 20 adult mites and inoculate them on the leaves of pepper. After 2 days, the adult mites are eliminated and the number of eggs of the mites is counted, and the leaves with eggs are immersed in the prepared liquid for 10 seconds. After taking out, the leaves are placed in a petri dish for moisturizing treatment.
  • test process is the same as above, the difference is that the virulence test is carried out on the eggs of Tetranychus cinnabarinus in different regions.
  • Bemisia tabaci eggs potted spray method, the original medicinal acetone was prepared into a mother liquor with a mass concentration of 1 wt % for standby use, and an aqueous solution of 0.1 wt % Tween 80 was used to prepare a test concentration.
  • a 0.1 wt% aqueous solution of Tween 80 was used as a blank control and placed in a 25°C worm breeding room. After the nymphs of the blank control group hatched, the number of nymphs in each treatment unit was counted, and the hatching inhibition rate was calculated.
  • Mosquito tartarii eggs The test was carried out by the quantitative drop method of the medicinal solution, and the original medicinal acetone was prepared into a mother solution with a mass concentration of 1 wt % and used for later use; the aqueous solution of 0.1 wt % Tween 80 was used to prepare the test concentration.
  • Pick the eggs of 2-day-old Mosquitoes tardigrades each treatment unit includes 20 eggs, put them into a petri dish with a diameter of 9 cm covered with filter paper, and add 600 microliters of liquid medicine on the eggs with a pipette. 600 microliters of drug solution on filter paper.
  • Each treatment was repeated 3 times, with 0.1 wt% Tween 80 aqueous solution as blank control, placed in a 24 ⁇ 1°C biochemical incubator after treatment, and the test results were checked on the 5th day after treatment.
  • Plutella xylostella eggs carry out the test using the leaf dipping method, prepare the original medicinal acetone into a mother liquor with a mass concentration of 1wt%, dilute it to the test concentration with deionized water containing 0.1wt% of Tween 80, and cultivate it in a diameter of 9 Pour 1.2% agar into the dish to cool down for later use; in the peak egg-laying stage of the adult diamondback moth, put 2 leaves and 1 heart of radish seedlings, take out 1 day later, select 20-30 radish seedlings with the number of eggs, immerse them in the liquid for 10 seconds and take them out , Put the radish seedlings in a petri dish for moisturizing treatment.
  • Corn armyworm eggs carry out the test by the leaf soaking method, prepare the original medicinal acetone into a mother liquor with a mass concentration of 1wt%, dilute it with deionized water containing 0.1wt% of Tween 80 to the test concentration for later use, and prepare it at a diameter of 9 cm. Pour 1.2% agar into the petri dish and cool it for later use; at the peak egg-laying stage of corn armyworm adults, put 2 leaves and 1 heart of corn seedlings, take them out after 1 day, select 20-30 corn leaves with the number of eggs, and immerse them in the liquid for 10 seconds After taking out, put the corn seedlings in a petri dish for moisturizing treatment.
  • Control object cinnabar spider mite
  • Test method The field efficacy test was carried out with reference to "Guidelines for Field Efficacy Test of Pesticide".
  • the test dose of the control agent is the recommended dose.
  • the clear water treatment was set as the blank control, and each dose of treatment was repeated 4 times and arranged in random blocks. Spray the chemical evenly on the front and back of the branches and leaves of the plant, so that the mites can fully contact the chemical liquid.
  • Investigate the base of insect population before spraying adopt fixed-point survey method after spraying, survey 2 plants in each plot, each plant is marked with five points in the east, south, west, north and middle, 1 shoot per point, 5 leaves per shoot, and 5 leaves per shoot. A total of 50 leaves were surveyed in the plot, and the number of live and nymph mites was recorded. The results of the survey were checked and recorded 14 days after the application, and the number of active mites on the leaves was checked and recorded, and the mite population reduction rate and the control effect of the treatment were calculated.
  • test drug Test concentration (mg/L) 14-day prevention effect (%) 5% trifluoromethyl emulsifiable concentrate 50 83.64 5% trifluoroacetate aqueous emulsion 50 79.21 5% trifluoromethyl ester water solution 50 85.32 5% trifluorosulfonate suspending agent 50 84.13 5% trifluorosulfonate microemulsion 50 79.77 110 g/L etoxazole suspension 50 56.79
  • Triflufenamide can effectively control Tetranychus cinnabarinus on cotton plants.
  • Control object two-spotted spider mite
  • Test method The field efficacy test was carried out with reference to "Guidelines for Field Efficacy Test of Pesticide".
  • the test dose of the control agent is the recommended dose.
  • the clear water treatment was set as the blank control, and each dose of treatment was repeated 4 times and arranged in random blocks. Spray the chemical evenly on the front and back of the branches and leaves of the plant, so that the mites can fully contact the chemical liquid.
  • Investigate the base of insect population before spraying adopt fixed-point survey method after spraying, survey 2 plants in each plot, each plant is marked with five points in the east, south, west, north and middle, 1 shoot per point, 5 leaves per shoot, and 5 leaves per shoot. A total of 50 leaves were surveyed in the plot, and the number of live and nymph mites was recorded. The results of the survey were checked and recorded 14 days after the application, and the number of active mites on the leaves was checked and recorded, and the mite population reduction rate and the control effect of the treatment were calculated.
  • test drug Test concentration (mg/L) 14-day prevention effect (%) 5% trifluoromethyl emulsifiable concentrate 50 83.26 5% trifluoroacetate aqueous emulsion 50 80.23 5% trifluoromethyl ester water solution 50 86.41 5% trifluorosulfonate suspending agent 50 85.33 5% trifluorosulfonate microemulsion 50 80.72 110 g/L etoxazole suspension 50 60.37
  • Control object citrus panclaw mite
  • Test method The field efficacy test was carried out with reference to "Guidelines for Field Efficacy Test of Pesticide".
  • the test dose of the control agent is the recommended dose.
  • the clear water treatment was set as the blank control, and each dose of treatment was repeated 4 times and arranged in random blocks. Spray the chemical evenly on the front and back of the branches and leaves of the plant, so that the mites can fully contact the chemical liquid.
  • test drug Test concentration (mg/L) 14-day prevention effect (%) 5% trifluoromethyl emulsifiable concentrate 50 80.21 5% trifluoroacetate aqueous emulsion 50 79.34 5% trifluoromethyl ester water solution 50 85.37 5% trifluorosulfonate suspending agent 50 83.45 5% trifluorosulfonate microemulsion 50 79.99 110 g/L etoxazole suspension 50 55.91
  • Triflunomide can effectively control Panonychus citrus mites on citrus plants.
  • Control object Hawthorn spider mites
  • Test method The field efficacy test was carried out with reference to "Guidelines for Field Efficacy Test of Pesticide".
  • the test dose of the control agent is the recommended dose.
  • the clear water treatment was set as the blank control, and each dose of treatment was repeated 4 times and arranged in random blocks. Spray the chemical evenly on the front and back of the branches and leaves of the plant, so that the mites can fully contact the chemical liquid.
  • test drug Test concentration (mg/L) 14-day prevention effect (%) 5% trifluoromethyl emulsifiable concentrate 50 79.08 5% trifluoroacetate aqueous emulsion 50 83.76 5% trifluoromethyl ester water solution 50 81.84 5% trifluorosulfonate suspending agent 50 88.83 5% trifluorosulfonate microemulsion 50 87.53 110 g/L etoxazole suspension 50 72.64
  • each preparation of the embodiment produces visible phytotoxic symptoms to the crops, and each crop after the application grows well, indicating that the triflufenac preparation can kill the insect eggs under the test concentration, In this way, the number of insect populations can be continuously reduced and the damage to crops can be reduced.

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  • Pest Control & Pesticides (AREA)
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Abstract

一种三氟杀线酯用于防治农业害虫、害螨的用途。三氟杀线酯可配置成农业上允许的乳油、水乳剂、水剂、可湿性粉剂、微乳剂、悬浮剂、微囊悬浮剂或水分散粒剂，其中三氟杀线酯在剂型中的含量为1％-80％。三氟杀线酯对农业害虫害螨防效突出，而且三氟杀线酯属于新化合物，与现有产品无交互抗性。

Description

三氟杀线酯用于防治农业害虫、害螨的用途
本发明要求2020年7月1日向中国国家知识产权局提交的，专利申请号为202010622002.X，发明名称为“三氟杀线酯用于防治农业害虫、害螨的用途”的在先申请的优先权，该在先申请的全文通过引用的方式结合于本发明中。
技术领域
本发明属于农业杀虫杀螨剂领域，涉及一种以三氟杀线酯为活性成分的用于防治农业害虫害螨的产品及其制备方法和用途。
背景技术
在作物栽培过程中，农业害虫害螨防治工作效果如何直接关系到作物的产量和质量。目前，化学防治是农业害虫害螨治理的重要措施之一，由于其高效、快速的优点，在未来的农业害虫害螨防治中仍然是其他防治方法不可替代的。但随着化学药剂的持续使用，农业害虫害螨的3R(抗性、再猖獗、残留)问题日渐突出，已成为公认的亟待解决的问题。
寻找安全、高效、与现有药剂无交互抗性的新型杀虫杀螨剂是解决农业害虫害螨防治过程中3R问题的最直接有效的方式。
发明内容
为了改善现有技术的不足，本申请的发明人发现三氟杀线酯对多种农业害虫害螨具有活性，能够有效抑制农业害虫害螨雌虫产卵，对害虫害螨卵活性突出，且三氟杀线酯与现有药剂无交互抗性，是解决农业害虫害螨3R问题的优良替代产品。三氟杀线酯(CAS：2074661-82-6)毒性级别为低毒，使用安全，属于环境友好型化合物。
本发明提供一种含有三氟杀线酯的杀虫杀螨剂，通过将有效量的杀虫杀螨剂施用于栖息、假定栖息或即将栖息害虫害螨的区域，主要通过抑制害虫害螨雌虫产卵，抑制害虫害螨卵孵化等方式减轻害虫害螨对作物的危害，同时对害虫害螨成虫和若虫也具有一定的杀死效果。
本发明目的是通过如下技术方案实现的：
三氟杀线酯用于防治农业害虫害螨的用途。
根据本发明，所述农业害虫害螨为植食性害螨、烟粉虱、迟眼蕈蚊、小菜蛾和粘虫(如玉米粘虫)中的至少一种。
根据本发明，所述植食性害螨为朱砂叶螨、二斑叶螨、柑橘全爪螨或山楂叶螨中的至少一种。
根据本发明，所述三氟杀线酯的结构如下所示：
Figure PCTCN2021099094-appb-000001
本发明还提供一种含三氟杀线酯的杀虫杀螨剂，所述含三氟杀线酯的杀虫杀螨剂包括三氟杀线酯和溶剂。
根据本发明，所述三氟杀线酯的加入量(杀虫杀螨剂中三氟杀线酯的质量)为1-80wt％，如1-60wt％，如1wt％、2wt％、5wt％、8wt％、10wt％、12wt％、15wt％、20wt％、25wt％、30wt％、35wt％、40wt％、45wt％、50wt％、55wt％、60wt％、70wt％或80wt％。
根据本发明，所述含三氟杀线酯的杀虫杀螨剂还包括乳化剂。
具体的，所述乳化剂的加入量(杀虫杀螨剂中乳化剂的质量)为3-30wt％，如3wt％、5wt％、8wt％、10wt％、12wt％、15wt％、20wt％、25wt％、28wt％或30wt％。
根据本发明，所述含三氟杀线酯的杀虫杀螨剂还可以包括其他助剂，所述其他助剂可以是增稠剂、防腐剂、消泡剂、分散剂、稳定剂、润湿剂、渗透剂和粘着剂等中的至少一种；所述其他助剂可以使所述含三氟杀线酯的杀虫杀螨剂制成针对不同使用场合，加工成农业上可使用的乳油、水乳剂、水剂、可湿性粉剂、微乳剂、悬浮剂、微囊悬浮剂或水分散粒剂。
示例性地，当本发明的作为防治农业害虫害螨产品(即含三氟杀线酯的杀虫杀螨剂)用于叶面喷雾及土壤处理使用的乳油时，其配方为：
三氟杀线酯：1-60wt％，
乳化剂：5-20wt％，
用混合溶剂补至100wt％。
其中，所述乳化剂选自农乳100#、TX-10、农乳500#、农乳602#、OP500、OP10、吐温80或农乳600#中的一种或多种，优选为5-8wt％的农乳100#、5-8wt％的农乳600#和3-8wt％的吐温80中的至少一种。
其中，所述混合溶剂为芳烃类溶剂油、乙酸乙酯或N-甲基吡咯烷酮中的两种以上的混合，其中优选芳烃类溶剂油:N-甲基吡咯烷酮＝1:1(V/V)。
生产过程：先加入混合溶剂，再投入定量称取的三氟杀线酯，加入乳化剂拌匀0.5小时充分均匀，再在配制罐中持续搅拌0.5小时。检测含量，分装于双重阻隔塑料瓶中，密封贮藏。
示例性地，当本发明的作为防治农业害虫害螨产品(即含三氟杀线酯的杀虫杀螨剂)用于叶面喷雾及土壤处理使用的水乳剂时，其配方为：
三氟杀线酯：1-50wt％，
乳化剂：12-28wt％，
溶剂：10-28wt％，
用水补至100wt％。
其中，所述乳化剂选自7780、7781T、4103、Well201、TX-10、农乳500#、农乳602#或WellM30等中一种或多种，优选乳化剂为5-15wt％的7780和3-12wt％的7781T。
其中，所述溶剂为芳香烃类溶剂或环已酮等。
生产过程：先加入溶剂，再投入定量称取的三氟杀线酯，加入乳化剂拌匀0.5小时充分均匀，再在配制罐中持续搅拌0.5小时。将混合液缓慢加入水中均质。检测含量，分装于双重阻隔塑料瓶中玻璃瓶或内涂阻隔层的铝瓶中，密封贮藏。
示例性地，当本发明的作为防治农业害虫害螨产品(即含三氟杀线酯的杀虫杀螨剂)用于叶面喷雾及土壤处理使用的水剂时，其配方为：
三氟杀线酯：1-80wt％，
乳化剂：12-28wt％，
用水补至100wt％。
其中，所述乳化剂为甜菜碱。
生产过程：先投入定量称取的三氟杀线酯，加入乳化剂，再加入水拌匀0.5小时 充分均匀，再在配制罐中持续搅拌0.5小时。检测含量，分装于双重阻隔塑料瓶中玻璃瓶或内涂阻隔层的铝瓶中，密封贮藏。
示例性地，当本发明的作为防治农业害虫害螨产品(即含三氟杀线酯的杀虫杀螨剂)用于叶面喷雾及土壤处理使用的悬浮剂时，其配方为：
三氟杀线酯：1-80wt％，
乳化剂：1-20wt％，
增稠剂：0.01-1wt％，
防腐剂：0.1-1wt％，
消泡剂：0.1-1wt％，
溶剂：1-10wt％，
用水补至100wt％。
其中，所述乳化剂为三苯乙烯基芬聚氧乙烯醚磷酸酯三乙醇铵盐、木质素磺酸盐或萘磺酸盐；所述增稠剂为黄原胶、硅酸镁铝或明胶；所述防腐剂为苯甲酸钠或苯甲酸；所述消泡剂选自有机硅类助剂，所述溶剂选自水、溶剂油、油酸甲酯、松脂油或碳酸丙烯酯。
生产过程：先将乳化剂、消泡剂、水混合均质，再投入定量称取的三氟杀线酯、溶剂，再均质砂磨。检测合格后加入防腐剂、增稠剂再均质，检测含量，分装于双重阻隔塑料瓶中玻璃瓶或内涂阻隔层的铝瓶中，密封贮藏。
示例性地，当本发明的作为防治农业害虫害螨产品(即含三氟杀线酯的杀虫杀螨剂)用于叶面喷雾及土壤处理使用的微乳剂时，其配方为：
三氟杀线酯：1-80wt％，
乳化剂：12-28wt％，
溶剂：1-10wt％，
用水补至100wt％。
其中，所述乳化剂为三苯乙烯基芬聚氧乙烯醚磷酸酯三乙醇铵盐或脂肪酸聚氧乙烯醚；所述溶剂选自水、溶剂油、油酸甲酯、松脂油、碳酸丙烯酯、环己酮或癸酰胺。
生产过程：先加入溶剂，再投入定量称取的三氟杀线酯，加入乳化剂拌匀0.5小时充分均匀，再在配制罐中持续搅拌0.5小时。再和水在配制罐中持续搅拌均匀。
本发明还提供一种防治农业害虫害螨的方法，所述方法包括如下步骤：
将上述含三氟杀线酯的杀虫杀螨剂通过叶面喷雾或土壤处理方式施用于害虫害 螨栖息、假定栖息或即将栖息害虫害螨的区域。
根据本发明，将上述含三氟杀线酯的杀虫杀螨剂通过叶面喷雾或土壤处理方式施用于害虫害螨卵栖息、假定栖息或即将栖息害虫害螨卵的区域。
本发明的有益效果：
本发明提供了一种三氟杀线酯用于防治农业害虫、害螨的用途。三氟杀线酯可配置成农业上允许的乳油、水乳剂、水剂、可湿性粉剂、微乳剂、悬浮剂、微囊悬浮剂或水分散粒剂，其中，三氟杀线酯在剂型中的含量为1％-80％。本发明中三氟杀线酯对农业害虫害螨防效突出，而且三氟杀线酯属于新化合物，与现有产品无交互抗性。
具体实施方式
下文将结合具体实施例对本发明做更进一步的详细说明。应当理解，下列实施例仅为示例性地说明和解释本发明，而不应被解释为对本发明保护范围的限制。凡基于本发明上述内容所实现的技术均涵盖在本发明旨在保护的范围内。
下述实施例中所使用的实验方法如无特殊说明，均为常规方法；下述实施例中所用的试剂、材料等，如无特殊说明，均可从商业途径得到。
下述实施例中所使用的螨口减退率及处理药剂防治效果(防效)的计算公式如下：
Figure PCTCN2021099094-appb-000002
Figure PCTCN2021099094-appb-000003
实施例1对植食性害螨毒力试验
产卵抑制活性测定试验：将原药用丙酮配制成质量浓度为1wt％的母液备用，用含0.1wt％的吐温80的去离子水稀释至试验系列浓度。分别选取新鲜的豇豆苗叶，并剪成直径约为5.0厘米的圆形叶碟，放置在铺有滤纸和脱脂棉的塑料培养皿中。用棉签在叶片背面分别涂上5、10毫克/升的处理药剂，采用相同的溶剂配比的水溶液作为对照药剂。待药液在室内条件下自然风干后，每张叶片接20头左右3～5日龄的雌成螨，每个处理重复5次，处理约100头螨。在相同饲养条件下放置，每隔24小时在双目解剖镜下观察并记录各处理的产卵量，连续观察6天。试验完毕，计算各处理的产卵抑制 率。
Figure PCTCN2021099094-appb-000004
螨卵孵化抑制活性测定试验：采用浸叶法开展试验，将原药用丙酮配制成质量浓度为1wt％的母液备用，用含0.1wt％的吐温80的去离子水稀释至试验系列浓度。在直径9厘米培养皿内倒入1.2％琼脂水冷却备用；挑选成螨20头接种到辣椒叶片上，2天后驱除成螨并统计螨卵数量，将带卵叶片浸入配制好的药液10秒后取出，将叶片放入培养皿中进行保湿处理。每个处理重复3次，以0.1wt％的吐温80的水溶液做空白对照，置于24±1℃生化培养箱内，待空白对照组若螨孵化完成后，检查试验结果，计算卵孵化率。
表1 三氟杀线酯对植食性害螨雌成螨产卵抑制活性测定试验
Figure PCTCN2021099094-appb-000005
结果如表1所示，可以看出，三氟杀线酯能够有效抑制4种雌成螨的产卵，减少产卵量。
表2 三氟杀线酯对植食性害螨卵的毒力测定试验
Figure PCTCN2021099094-appb-000006
结果如表2所示，可以看出，三氟杀线酯对4种植食性害螨卵均具有突出活性。
测试过程同上，区别在于分别在不同地区的朱砂叶螨卵进行毒力测试。
表3 三氟杀线酯对不同地区朱砂叶螨卵的毒力测定试验
Figure PCTCN2021099094-appb-000007
结果如表3所示，可以看出，三氟杀线酯对各地区朱砂叶螨卵活性比较稳定，不同于乙螨唑随着地区的不同，活性出现变化，可以推测三氟杀线酯与乙螨唑无交互抗性，通过相同试验方法进行三氟杀线酯与市售杀螨剂产品进行对比，可推测三氟杀线酯与现有杀螨剂无交互抗性。
实施例2对其他农业害虫卵活性
烟粉虱卵：盆栽喷雾法，将原药用丙酮配制成质量浓度为1wt％的母液备用，用0.1wt％的吐温80的水溶液配制成试验浓度。选取长势一致的辣椒盆栽，每6棵辣椒盆栽为一个处理单元，放入养虫笼中，每个养虫笼内接入500头左右烟粉虱，正常管理2天后驱赶成虫；药剂配制完成后，对辣椒植株进行喷雾处理，喷雾后置于养虫笼内。 以0.1wt％的吐温80的水溶液做空白对照，置于25℃养虫室中，待空白对照组若虫孵化完成后，统计各处理单元的若虫数，计算孵化抑制率。
迟眼蕈蚊卵：采用药液定量滴加法开展试验，将原药用丙酮配制成质量浓度为1wt％的母液后备用；用0.1wt％的吐温80的水溶液配制成试验浓度。挑取2日龄的迟眼蕈蚊卵，每个处理单元包括20粒卵，放入铺有滤纸的直径9厘米的培养皿中，用移液枪滴加600微升药液于卵上，600微升药液于滤纸上。每个处理重复3次，以0.1wt％的吐温80的水溶液做空白对照，处理后置于24±1℃生化培养箱内，药后第5天检查试验结果。
表4 三氟杀线酯对其他农业害虫卵毒力测定试验结果
Figure PCTCN2021099094-appb-000008
结果如表4所示，可以看出，三氟杀线酯对测试2种农业害虫卵均具有突出效果。
实施例3对其他农业害虫卵活性
小菜蛾卵：采用浸叶法开展试验，将原药用丙酮配制成质量浓度为1wt％的母液，用含0.1wt％的吐温80的去离子水稀释至试验浓度备用，在直径9里面培养皿内倒入1.2％琼脂冷却备用；在小菜蛾成虫产卵盛期，放入2叶1心萝卜苗，1天后取出，选取卵数量20～30头萝卜苗，浸入药液中10秒后取出，将萝卜苗放入培养皿中进行保湿处理。每个处理重复3次，以0.1wt％的吐温80的水溶液做空白对照，置于25℃养虫室中，待空白对照组的幼虫孵化完成后，检查试验结果，计算孵化率。
玉米粘虫卵：采用浸叶法开展试验，将原药用丙酮配制成质量浓度为1wt％的母液，用含0.1wt％的吐温80的去离子水稀释至试验浓度备用，在直径9厘米培养皿内倒入1.2％琼脂冷却备用；在玉米粘虫成虫产卵盛期，放入2叶1心玉米苗，1天后取出，选取卵数量20～30头玉米叶，浸入药液中10秒后取出，将玉米苗放入培养皿中进行保湿处理。每个处理重复3次，以0.1wt％的吐温80的水溶液做空白对照，置于25℃养虫 室中，待空白对照组的幼虫孵化完成后，检查试验结果，计算孵化率。
表5 三氟杀线酯对其他农业害虫卵毒力测定试验结果
Figure PCTCN2021099094-appb-000009
结果如表5所示，可以看出，三氟杀线酯对测试2种农业害虫卵均具有突出效果。
实施例4田间药效试验
试验作物：棉花
防治对象：朱砂叶螨
试验方法：田间药效试验参照《农药田间药效试验准则》进行。对照药剂试验剂量为推荐剂量。设清水处理为空白对照，每个剂量处理4次重复，随机区组排列。将药剂均匀喷雾于植株枝条和叶片正反面，使螨充分接触药液。施药前调查虫口基数，施药后采用定点调查法，每小区调查2株植株，每株标记东、南、西、北、中五点，每点1梢，每梢调查5张叶片，每小区共调查50张叶片，记录活成、若螨数，于施药后14天调查结果，检查并记录叶片上活动态螨的数量，计算螨口减退率及处理药剂防治效果。
表6 三氟杀线酯对朱砂叶螨田间防效试验结果
供试药剂 试验浓度(mg/L) 14天防效(％)
5％三氟杀线酯乳油 50 83.64
5％三氟杀线酯水乳剂 50 79.21
5％三氟杀线酯水剂 50 85.32
5％三氟杀线酯悬浮剂 50 84.13
5％三氟杀线酯微乳剂 50 79.77
110克/升乙螨唑悬浮剂 50 56.79
结果如表6所示，三氟杀线酯能够有效防除棉花植株上的朱砂叶螨。
实施例5田间药效试验
试验作物：黄瓜
防治对象：二斑叶螨
试验方法：田间药效试验参照《农药田间药效试验准则》进行。对照药剂试验剂量为推荐剂量。设清水处理为空白对照，每个剂量处理4次重复，随机区组排列。将药剂均匀喷雾于植株枝条和叶片正反面，使螨充分接触药液。施药前调查虫口基数，施药后采用定点调查法，每小区调查2株植株，每株标记东、南、西、北、中五点，每点1梢，每梢调查5张叶片，每小区共调查50张叶片，记录活成、若螨数，于施药后14天调查结果，检查并记录叶片上活动态螨的数量，计算螨口减退率及处理药剂防治效果。
表7 三氟杀线酯对二斑叶螨田间防效试验结果
供试药剂 试验浓度(mg/L) 14天防效(％)
5％三氟杀线酯乳油 50 83.26
5％三氟杀线酯水乳剂 50 80.23
5％三氟杀线酯水剂 50 86.41
5％三氟杀线酯悬浮剂 50 85.33
5％三氟杀线酯微乳剂 50 80.72
110克/升乙螨唑悬浮剂 50 60.37
结果如表7所示，三氟杀线酯能够有效防除黄瓜植株上二斑叶螨。
实施例6田间药效试验
试验作物：柑橘
防治对象：柑橘全爪螨
试验方法：田间药效试验参照《农药田间药效试验准则》进行。对照药剂试验剂量为推荐剂量。设清水处理为空白对照，每个剂量处理4次重复，随机区组排列。将药剂均匀喷雾于植株枝条和叶片正反面，使螨充分接触药液。施药前调查虫口基数，施药后采用定点调查法，每小区调查2株植株，每株标记东、南、西、北、中五点，每点1梢，每梢调查5张叶片，每小区共调查50张叶片，记录活成、若螨数，于施药后14天调查结果，检查并记录叶片上活动态螨的数量，计算螨口减退率及处理药剂防治 效果。
表8 三氟杀线酯对柑橘全爪螨田间防效试验结果
供试药剂 试验浓度(mg/L) 14天防效(％)
5％三氟杀线酯乳油 50 80.21
5％三氟杀线酯水乳剂 50 79.34
5％三氟杀线酯水剂 50 85.37
5％三氟杀线酯悬浮剂 50 83.45
5％三氟杀线酯微乳剂 50 79.99
110克/升乙螨唑悬浮剂 50 55.91
结果如表8所示，三氟杀线酯能够有效防除柑橘植株上的柑橘全爪螨。
实施例7田间药效试验
试验作物：山楂
防治对象：山楂叶螨
试验方法：田间药效试验参照《农药田间药效试验准则》进行。对照药剂试验剂量为推荐剂量。设清水处理为空白对照，每个剂量处理4次重复，随机区组排列。将药剂均匀喷雾于植株枝条和叶片正反面，使螨充分接触药液。施药前调查虫口基数，施药后采用定点调查法，每小区调查2株植株，每株标记东、南、西、北、中五点，每点1梢，每梢调查5张叶片，每小区共调查50张叶片，记录活成、若螨数，于施药后14天调查结果，检查并记录叶片上活动态螨的数量，计算螨口减退率及处理药剂防治效果。
表9 三氟杀线酯对山楂叶螨田间防效试验结果
供试药剂 试验浓度(mg/L) 14天防效(％)
5％三氟杀线酯乳油 50 79.08
5％三氟杀线酯水乳剂 50 83.76
5％三氟杀线酯水剂 50 81.84
5％三氟杀线酯悬浮剂 50 88.83
5％三氟杀线酯微乳剂 50 87.53
110克/升乙螨唑悬浮剂 50 72.64
结果如表9所示，三氟杀线酯能够有效防除山楂叶螨。
在施药到调查结束观察，均未发现实施例各制剂对作物产生可见的植物毒性症 状，施药后的各作物生长良好，说明在试验浓度下三氟杀线酯制剂能够灭杀害虫卵，从而持续降低虫口数量，减轻对作物的危害。
应当理解的是，上述实施例是本发明的部分实施例，仅仅是为了更好的了解本发明的实施例而提供的，并不是本发明的所有实施例。实际应用中，通过调整本发明中上述各个组分的含量以及组分之间的组合方式，可以获得不同的、无数的实施例，这些均在本发明的涵盖范围内。
以上，对本发明的实施方式进行了说明。但是，本发明不限定于上述实施方式。凡在本发明的精神和原则之内，所做的任何修改、等同替换、改进等，均应包含在本发明的保护范围之内。

Claims (10)

  1. 三氟杀线酯用于防治农业害虫害螨的用途。
  2. 根据权利要求1所述的用途，其中，所述农业害虫害螨为植食性害螨、烟粉虱、迟眼蕈蚊、小菜蛾和粘虫中的至少一种。
  3. 根据权利要求2所述的用途，其中，所述植食性害螨为朱砂叶螨、二斑叶螨、柑橘全爪螨或山楂叶螨中的至少一种。
  4. 一种含三氟杀线酯的杀虫杀螨剂，其中，所述含三氟杀线酯的杀虫杀螨剂包括三氟杀线酯和溶剂。
  5. 根据权利要求4所述的含三氟杀线酯的杀虫杀螨剂，其中，所述三氟杀线酯的加入量为1-80wt％，如1-60wt％。
  6. 根据权利要求4或5所述的含三氟杀线酯的杀虫杀螨剂，其中，所述含三氟杀线酯的杀虫杀螨剂还包括乳化剂，所述乳化剂的加入量为3-30wt％。
  7. 根据权利要求4-6任一项所述的含三氟杀线酯的杀虫杀螨剂，其中，所述含三氟杀线酯的杀虫杀螨剂还包括其他助剂，所述其他助剂是增稠剂、防腐剂、消泡剂、分散剂、稳定剂、润湿剂、渗透剂和粘着剂中的至少一种。
  8. 根据权利要求4-7任一项所述的含三氟杀线酯的杀虫杀螨剂，其中，所述含三氟杀线酯的杀虫杀螨剂是乳油、水乳剂、水剂、可湿性粉剂、微乳剂、悬浮剂、微囊悬浮剂或水分散粒剂。
  9. 一种防治农业害虫害螨的方法，其中，所述方法包括如下步骤：
    将权利要求4-8任一项所述的含三氟杀线酯的杀虫杀螨剂通过叶面喷雾或土壤处理方式施用于害虫害螨栖息、假定栖息或即将栖息害虫害螨的区域。
  10. 根据权利要求9所述的方法，其中，将权利要求4-8任一项所述的含三氟杀线酯的杀虫杀螨剂通过叶面喷雾或土壤处理方式施用于害虫害螨卵栖息、假定栖息或即将栖息害虫害螨卵的区域。
PCT/CN2021/099094 2020-07-01 2021-06-09 三氟杀线酯用于防治农业害虫、害螨的用途 WO2022001601A1 (zh)

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