Insecticidal and acaricidal composition
By using a specific ratio of active components A and B in an insecticide and acaricide, the problem of pest resistance caused by a single active component is solved, achieving efficient and low-dose pest control, and reducing environmental pollution and costs.
Patent Information
- Application Number
- PCT/CN2025/109324
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-07-20
- Filing Date
- 2025-07-18
- Publication Date
- 2026-01-29
AI Technical Summary
Existing single-active-component insecticides and acaricides are prone to leading to pesticide resistance in pests with long-term use, and existing mixture options cannot effectively delay the development of resistance, failing to meet the needs of agriculture, forestry, and urban sanitation sectors for highly effective, low-dose, and environmentally friendly insecticides and acaricides.
An insecticidal and acaricidal composition is provided, wherein active component A and active component B are mixed in a specific ratio. Component A is selected from various insecticidal and acaricidal agent categories, and component B is selected from biomimetic juvenile hormones, chitin biosynthesis inhibitors, etc. The ratio of active components in the composition is 1:100-100:1, and different formulations are prepared for agricultural and urban pest control.
It delays the development of pesticide resistance in pests, improves the control effect on resistant populations, enhances insecticidal and acaricidal effects, reduces dosage and cost, and reduces environmental pollution.
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Figure CN2025109324_29012026_PF_FP_ABST
Abstract
Description
Insecticidal and acaricidal composition
[0001] Cross-references to related applications
[0002] This application claims the benefit of Chinese patent applications 202410976327.6, 202410976331.2, 202410976335.0, 202410976336.5, 202410976338.4, and 202410976342.0, all filed on July 20, 2024, the contents of which are incorporated herein by reference. Technical Field
[0003] This invention belongs to the field of insecticides and acaricides, and relates to insecticide and acaricide compositions. Background Technology
[0004] In agricultural and horticultural crop production, damage caused by pests and diseases remains significant. Due to biodiversity and the simultaneous occurrence of multiple pests and diseases, the field of plant protection has a continuous need to develop new insecticides and acaricides with better activity, lower dosage, and greater environmental friendliness. Continuous use of insecticides and acaricides containing a single active ingredient in pest control easily leads to pesticide resistance. Blending insecticides and acaricides with two or more active ingredients into mixed formulations plays an important role in broadening the insecticidal spectrum, controlling both pests and diseases, controlling viral diseases by controlling vector insects, and reducing pesticide application costs for farmers. It can also delay the development of pesticide resistance in pests. Although mixtures can delay resistance, the choice of two substances cannot be guaranteed. Summary of the Invention
[0005] In view of the shortcomings of the existing technology, the purpose of this invention is to provide an insecticidal and acaricidal composition to meet the increasing demand for insecticides and acaricides in the fields of agricultural and forestry and urban sanitation for pest control, which are characterized by increasingly improved efficacy and continuous updates in the variety of insecticides and acaricides.
[0006] To achieve the above objectives, the technical solution adopted by the present invention is as follows:
[0007] This invention provides an insecticidal and acaricidal composition containing active component A and active component B, wherein the weight ratio of active component A to active component B is 1:100-100:1; wherein active component B is selected from biomimetic juvenile hormones, chitin biosynthesis inhibitors affecting CHS1, chitin biosynthesis inhibitor type 1, ecdysone receptor agonists, nicotinic acetylcholine receptor competitive modulators, ryanodine receptor modulators, nicotinic acetylcholine receptor allosteric modulators, glutamate-gated chloride channel allosteric modulators, sodium channel modulators, and electrolytic... The active ingredient A is selected from one or more of the following: pressure-dependent sodium channel blockers, inhibitors affecting chitin synthase 1 in mites, mitochondrial adenosine triphosphate synthase inhibitors, mitochondrial electron transport complex (III) inhibitors, mitochondrial electron transport complex (I) inhibitors, acetyl-CoA carboxylase inhibitors, mitochondrial electron transport complex (II) inhibitors, trifluoroethyl sulfide acaricides, and other insecticides and acaricides; the active ingredient A is selected from compound I, compound II, or their stereoisomers, and the structures of compound I, compound II, or their stereoisomers are as follows:
[0008] In some embodiments, the weight ratio between active component A and active component B is 1:99-99:1, for example, 1:99, 1:90, 1:80, 1:70, 1:60, 1:50, 1:40, 1:30, 1:20, 1:10, 1:8, 1:5, 1:4, 1:3, 1:2, 1:1, 2:1, 3:1, 4:1, 5:1, 8:1, 10:1, 20:1, 30:1, 40:1, 50:1, 60:1, 70:1, 80:1, 90:1, 99:1, and any value within the range of any two values, preferably 1:80-80:1.
[0009] In some embodiments, the biomimetic juvenile hormone is selected from one or more of acetamiprid, acetamiprid, phenoxycarb, and pyriproxyfen.
[0010] In some typical implementations, the biomimetic juvenile hormone is selected from pyriproxyfen.
[0011] In some embodiments, the chitin biosynthesis inhibitors affecting CHS1 are selected from one or more of diflubenzuron, flucyclopropionate, fenflurfen, flufenoxuron, and fluorophenylurea.
[0012] In some typical implementations, the chitin biosynthesis inhibitors affecting CHS1 are selected from lufenuron.
[0013] In some embodiments, the chitin biosynthesis inhibitor type 1 is selected from thiamethoxam and / or cyromazine.
[0014] In some typical implementations, the chitin biosynthesis inhibitor type 1 is selected from thiamethoxam.
[0015] In some embodiments, the ecdysone receptor agonist class is selected from one or more of cyclotetracycline, chlorfenapyr, methoxyfenozide, and tebufenozide.
[0016] In some typical implementations, the ecdysone receptor agonist class is selected from methoxyfenozide.
[0017] In some embodiments, the nicotinic acetylcholine receptor (nAChR) competitive modulator is selected from one or more of chlorpyrifos, thiamethoxam, acetamiprid, fipronil, thiamethoxam, acetamiprid, thiamethoxam, chlorothiazoline, flonicamid, piperazine, sulfadiazine, nicotine, flonicamid, flupyrflufenoxuron, trifluoropyrimidine, dichlorothiapyrimidine, and fipronil.
[0018] In some typical embodiments, the nicotinic acetylcholine receptor (nAChR) competitive modulator is selected from one or more of imidacloprid, flonicamid, and trifluoropyrimidine.
[0019] In some embodiments, the ryanodine receptor modulators are selected from at least one of flubendiamide, chlorantraniliprole, cyclobromhizolide, tetrazolium benzoate, chlorantraniliprole, broflanilide, and chlorfluazuron, that is, the ryanodine receptor modulators may be selected from one or more of flubendiamide, cyclobromhizolide, tetrazolium benzoate, chlorantraniliprole, broflanilide, and chlorfluazuron.
[0020] In some typical implementations, the ryanodine receptor modulators are selected from chlorantraniliprole and / or bromocyanamide.
[0021] In some embodiments, the nicotinic acetylcholine receptor (nAChR) allosteric modulators are selected from ethyl spinosad and / or spinosad.
[0022] In some typical implementations, the nicotinic acetylcholine receptor (nAChR) allosteric modulator is selected from spinosad.
[0023] In some embodiments, the glutamate-gated chloride channel (GluCl) allosteric modulator is selected from one or more of avermectin, emamectin benzoate, rapamectin, and mibamectin.
[0024] In some typical implementations, the glutamate-gated chloride channel (GluCl) allosteric modulators are selected from avermectin.
[0025] In some embodiments, the sodium channel modulator is selected from cypermethrin, lambda-cyhalothrin, fenpropathrin, fenvalerate, flucythrinate, flumethrin, beta-cyfluthrin, cyfluthrin, bifenthrin, deltamethrin, acridine lactate, and cis-cypermethrin. Alpha-cypermethrin, bifenthrin, cyhalothrin, permethrin, fluvalinate, allethrin, bioallethrin, cycloprothrin, gamma-cyhalothrin, theta-cypermethrin, zeta-cypermethrin, cypheline Nothrin, empenthrin, esfenvalerate, imiprothrin, meperfluthrin, metofluthrin, dimefluthrin, prallethrin, phenothrin, resmethrin, bioresmethrin, cismethrin, tefluthrin, tetr amethrin, tetramethylfluthrin, tralomethrin, beta-cypermethrin, ethofenprox, transfluthrin, esdépalléthrine, barthrin, bioethanomethrin, brofenvalerate, brofluthrinate, bromethrin, butethrinChlorempenthrin, Cycyclethrin, Cyhalothrin, Lambda-Cyhalothrin, Dimethrin, D-Fanshiluquebingjuzhi, Fenfluthrin, Fenpirithrin, S-Cypermethrin, Furamethrin, Imiprothrin, Japothrins, Kadethrin, Methothrin, Penmethrin, Biopermethrin, Methionylpyrethrin One or more of the following: proparthrin, resmethrin, terallethrin, tralocythrin, valerate, flufenprox, halfenprox, sulfoxime, thiofluoximate, flumethrin, furthrin, heptafluthrin, momfluorothrin, transpermethrin, profluthrin, pyresmethrin, protrifenbute, silafluofen, DDT, and methoxydichlorophenoxyacetic acid (DDT).
[0026] In some typical implementations, the sodium channel modulator is selected from cypermethrin.
[0027] In some embodiments, the voltage-dependent sodium channel blocker is selected from indoxacarb and / or cyfluthrin.
[0028] In some typical implementations, the voltage-dependent sodium channel blocker is selected from indoxacarb.
[0029] In some embodiments, the inhibitors affecting the growth of chitin synthase 1 (CHS1) mites are selected from one or more of tetradifon, flufenoxuron, thiamethoxam, and etoxazole.
[0030] In some typical implementations, the inhibitors affecting the growth of chitin synthase 1 (CHS1) mites are selected from etoxazole.
[0031] In some embodiments, the mitochondrial adenosine triphosphate (ATP) synthase inhibitors are selected from one or more of bufenozide, triazole tin, tricyclic tin, phenylbutazone, propargite, and trichlorfon.
[0032] In some typical implementations, the mitochondrial adenosine triphosphate (ATP) synthase inhibitors are selected from bufenozide and / or propargite.
[0033] In some embodiments, the mitochondrial electron transport complex (III) inhibitors are selected from one or more of flufenoxuron, cypermethrin, pyrimethanil, and bifenazate.
[0034] In some typical implementations, the mitochondrial electron transport complex (III) inhibitors are selected from biphenylhydrazine esters.
[0035] In some embodiments, the mitochondrial electron transport complex (I) inhibitors are selected from one or more of quinclorac, azoxystrobin, pyridaben, pyrimethanil, pyridaben, tebufenozide, and rotenone.
[0036] In some typical implementations, the mitochondrial electron transport complex (I) inhibitors are selected from pyridaben.
[0037] In some embodiments, the acetyl-CoA carboxylase inhibitors are selected from one or more of spirodiclofen, spirodiclofen, methoxypiperidine ethyl ester, and spirotetramat.
[0038] In some typical implementations, the acetyl-CoA carboxylase inhibitors are selected from spirodiclofen and / or spirodiclofen.
[0039] In some embodiments, the mitochondrial electron transport complex (II) inhibitors are selected from one or more of pyridaben, etoxazole, dicofol, and pyrazolyl aniline;
[0040] In some typical implementations, the mitochondrial electron transport complex (II) inhibitors are selected from etoxazole.
[0041] In some embodiments, the trifluoroethyl sulfide acaricide is selected from one or more of bentioflumin, bisulflufen, flufenox, sulfiflumin, and flupentiofenox.
[0042] In some typical implementations, the trifluoroethyl sulfide acaricide is selected from bentioflumin.
[0043] In some implementations, other acaricides are selected from one or more of azadirachtin, cryolite, boric acid, thiocyanate, bensulfuron-methyl, pyrimethanil, sulfafuran sodium, amitraz, and veratrine.
[0044] In some typical implementation schemes, other types of acaricides are selected from veratrine.
[0045] In some embodiments, the active component B is selected from one or more of pyriproxyfen, lufenuron, thiamethoxam, and methoxyfenozide.
[0046] In some embodiments, the weight ratio of active component A to active component B is 1:60-30:1.
[0047] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from pyriproxypyridine; the weight ratio of the two active components is 1:50-30:1, preferably 1:30-30:1.
[0048] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from lufenuron; the weight ratio of the two active components is 1:50-30:1, preferably 1:50-20:1.
[0049] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from thiamethoxam; the weight ratio of the two active components is 1:50-30:1, preferably 1:50-20:1.
[0050] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from methoxyfenozide; the weight ratio of the two active components is 1:50-30:1, preferably 1:50-20:1.
[0051] In some embodiments, the active component B is selected from one or more of imidacloprid, flonicamid, and trifluorophenylpyrimidine.
[0052] In some embodiments, the weight ratio of active component A to active component B is 1:80-30:1.
[0053] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from imidacloprid; the weight ratio of the two active components is 1:30-30:1.
[0054] In some embodiments, the active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from flonicamid; the weight ratio of the two active components is 1:80-20:1, preferably 1:40-5:1, and more preferably 1:4.
[0055] In some embodiments, the active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from trifluorophenylpyrimidine; the weight ratio of the two active components is 1:80-20:1, preferably 1:50-20:1, and more preferably 1:2.
[0056] In some embodiments, the active component B is selected from chlorantraniliprole and / or bromocyanamide.
[0057] In some embodiments, the weight ratio of active component A to active component B is 1:80-80:1.
[0058] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from chlorantraniliprole; the weight ratio of the two active components is 1:80-80:1, preferably 1:20-20:1, and more preferably 1:4.
[0059] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from bromocyanamide; the weight ratio of the two active components is 1:50-50:1, preferably 1:30-30:1, more preferably 1:10-10:1, and even more preferably 1:2.
[0060] In some embodiments, the active component B is selected from ethyl spinosad and / or avermectin.
[0061] In some embodiments, the weight ratio of active component A to active component B is 1:80-100:1.
[0062] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from ethyl spinosad; the weight ratio of the two active components is 1:30-30:1, preferably 1:20-20:1, and more preferably 1:2.
[0063] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from avermectin; the weight ratio of the two active components is 1:80-100:1, preferably 1:30-30:1, and more preferably 1:2-4:1.
[0064] In some embodiments, the active ingredient B is selected from cypermethrin and / or indoxacarb.
[0065] In some embodiments, the weight ratio of active component A to active component B is 1:80-40:1.
[0066] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from cypermethrin; the weight ratio of the two active components is 1:80-40:1, preferably 1:80-30:1.
[0067] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from indoxacarb; the weight ratio of the two active components is 1:40-30:1.
[0068] In some embodiments, the active component B is selected from one or more of etoxazole, veratrine, pyridaben, propargite, bifenazate, spirodiclofen, etoxazole, and benzimidazole.
[0069] In some embodiments, the weight ratio of active component A to active component B is 1:100-30:1.
[0070] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from etoxazole; the weight ratio of the two active components is 1:30-30:1.
[0071] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from veratrine; the weight ratio of the two active components is 1:30-30:1.
[0072] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from pyridaben; the weight ratio of the two active components is 1:30-30:1.
[0073] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from butyl ether urea or propargite; the weight ratio of the two active components is 1:100-30:1, preferably 1:80-30:1.
[0074] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from biphenylhydrazine ester; the weight ratio of the two active components is 1:80-30:1, preferably 1:30-30:1, and more preferably 1:15.
[0075] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from spirodiclofen or spirodiclofen; the weight ratio of the two active components is 1:30-30:1, preferably 1:25-4:1.
[0076] In some embodiments, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from etoxazole nitrile; the weight ratio of the two active components is 1:30-30:1, preferably 1:20-20:1, and more preferably 1:2.
[0077] In some embodiments, the active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from benzylpyridinium; the weight ratio of the two active components is 1:40-20:1, preferably 1:4.
[0078] Further, the composition is mixed with a carrier and any one of the adjuvants to prepare a formulation containing the composition. The cumulative content of the active ingredient in the formulation is between 0.5 wt% and 95 wt%. Preferably, the cumulative content of the active ingredient in the formulation is between 1% and 85%.
[0079] The carrier described in this invention can be solid or liquid, and any carrier commonly used for formulating pesticide compositions can be used.
[0080] In this invention, suitable solid carriers include: minerals, plant materials, synthetic fillers, and inorganic salts. Minerals include silicates, carbonates, sulfates, and oxides. Examples of silicates include kaolin, sepiolite, perlite, montmorillonite, mica, vermiculite, pyrophyllite, and talc. Examples of carbonates include calcium carbonate and dolomite. Examples of sulfates include ammonium sulfate, sodium sulfate, and calcium sulfate. Examples of oxides include quicklime, magnesia lime, and diatomaceous earth. Examples of plant materials include citrus pomace, corncob, rice husk powder, rice husk, soybean straw powder, tobacco powder, walnut shells, and sawdust. Examples of synthetic fillers include precipitated calcium carbonate hydrate, precipitated calcium carbonate, and silica. Examples of inorganic salts include potassium chloride and sodium chloride.
[0081] In this invention, the liquid carrier includes water and an organic solvent. When the active ingredient is a suspension emulsion, the organic solvent acts as a solubilizer and antifreeze agent. Suitable organic solvents include aromatic hydrocarbons, such as benzene, xylene, toluene, alkylbenzenes, alkylnaphthalenes, and chlorinated aromatic hydrocarbons; chlorinated aliphatic hydrocarbons, such as vinyl chloride, chloroform, dichloromethane, chloroform, carbon tetrachloride, and polychloroethanes; aliphatic hydrocarbons, such as petroleum fractions, cyclohexane, light mineral oils, and paraffin waxes. Alcohols include methanol, ethanol, isopropanol, butanol, isobutanol, ethylene glycol, propylene glycol, glycerol, and fatty alcohols; ethers include methyl ethylene glycol ether, ethyl ethylene glycol ether, and petroleum ether; ketones include acetone, methyl ethyl ketone, methyl isobutyl ketone, cyclohexanone, isoflurane, and N-methylpyrrolidone; special solvents also include dimethylformamide, dimethyl sulfoxide, polyethylene glycol, and hexanilide; vegetable oils and methylated vegetable oils. The above-mentioned organic solvents can be used alone, in combination, or mixed with water.
[0082] In this invention, the additives may include one or more of surfactants, defoamers, thickeners, suspending agents and antifreeze agents as needed, and may also include other additives commonly used in this industry as needed.
[0083] In this invention, the surfactant can be an emulsifier, dispersant, stabilizer, or wetting agent; it can be ionic or nonionic. Suitable surfactants include: sodium and calcium salts of polyacrylic acid and lignin sulfonate; condensation products of fatty acids or fatty amines containing at least 12 carbon atoms with ethylene oxide and / or propylene oxide; fatty acid esters of glycerol, dodecyl-1, tetradecyl-1, sorbitol, sucrose, or pentaerythritol; and their condensation products with ethylene oxide and / or propylene oxide; sulfates or sulfonates of their condensation products; alkali metal or alkaline earth metal salts of sulfuric acid or sulfonic acid containing at least 10 carbon atoms, preferably sodium salts, such as sodium dodecyl sulfate, sodium secondary alkyl sulfate, sodium salt of sulfonated castor oil, sodium alkylaryl sulfonate, and sodium dodecylbenzene sulfonate; polymers of ethylene oxide, and copolymers of ethylene oxide and propylene oxide.
[0084] In this invention, the emulsifiers include nonionic and anionic emulsifiers. Preferred nonionic emulsifiers are nonylphenol polyoxyethylene ether, fatty alcohol polyoxyethylene ether, styrene-phenyl polyoxyethylene ether, alkylphenol formaldehyde resin polyoxyethylene ether, hydroxyl-terminated polyoxyethylene polyoxypropylene ether, styrene-phenol formaldehyde resin polyoxyethylene polyoxypropylene ether, and castor oil polyoxyethylene ether. Anionic emulsifiers mainly include calcium dodecylbenzenesulfonate, triphenylethylphenol polyoxyethylene ether phosphate amine salt, nonylphenol polyoxyethylene ether phosphate amine salt, and castor oil polyoxyethylene ether phosphate amine salt.
[0085] In this invention, the dispersant includes one or more of the following: sodium salt of acrylic acid homopolymer, disodium salt of maleate, sodium salt of naphthalene sulfonate formaldehyde condensate, rosin block polyoxyethylene ether polyoxypropylene ether sulfonate, hydroxyl-terminated polyoxyethylene polyoxypropylene ether block copolymer, triphenylethylphenol polyoxyethylene ether phosphate, fatty alcohol polyoxyethylene ether phosphate, and sodium p-hydroxyphenyl lignin sulfonate.
[0086] The wetting agent of the present invention includes one or more of the following: fatty alcohol polyoxyethylene ether, naphthalene sulfonate, sodium dodecyl sulfate, and alkylphenol resin polyoxyethylene ether sulfate.
[0087] The thickeners described in this invention include one or more of xanthan gum, magnesium aluminum silicate, sodium alginate, sodium carboxymethyl cellulose, gum arabic, gelatin, and polyvinyl alcohol.
[0088] The defoaming agents described in this invention include foam inhibitors, silicones, C8-10 fatty alcohols, C10-20 saturated fatty acids, and amides, etc.
[0089] The fungicides and insecticides described in this invention can be formulated into any agriculturally permissible formulation as needed, such as powder formulations, granular formulations, dispersible powder formulations, dispersible granular formulations, dispersible tablet formulations, soluble solid formulations, soluble liquid formulations, oil formulations, ultra-low volume formulations, dispersible liquid formulations, emulsion formulations, suspension formulations, suspension emulsions, or seed coating agents.
[0090] The present invention also provides an application of an insecticidal and acaricidal composition in the preparation of an insecticidal and acaricidal agent for controlling agricultural pests or urban sanitation pests.
[0091] In this invention, agricultural pests include armyworms, beet armyworms, cotton bollworms, cutworms, cabbage armyworms, apple leafrollers, rice leaf rollers, corn borers, rice stem borers, diamondback moths, cabbage caterpillars, fall webworms, tent caterpillars, gypsy moths, migratory locusts, underground pests, leaf miners, leaf miners, aphids, leafhoppers, flower scale insects, potato beetles, flea beetles, thrips, mirid bugs, carmine spider mites, hawthorn spider mites, citrus rust mites, apple spider mites, two-spotted spider mites, gall mites, flour mites, etc., while urban pests include termites, cockroaches, ants, flies, mosquitoes, etc. When used to control agricultural pests, it can be applied to fruit trees, cereals, legumes, vegetables, and flowers. Specifically, it can be used on fruit trees such as apples, pears, citrus fruits, and lychees; cereals such as wheat and rice; legumes such as soybeans and kidney beans; cotton; and vegetables such as cabbage, cauliflower, Chinese cabbage, rapeseed, tomatoes, and peppers. When used to control urban pests, it can be applied to homes, various public places, offices, and trees and embankments infested with termites.
[0092] Furthermore, the present invention provides a method for using an insecticidal and acaricidal composition, wherein the prepared insecticidal and acaricidal agent is applied to the pests to be controlled or their growth medium, in an effective dose. A generally suitable effective dose is typically selected to be 10 to 500 grams per hectare, preferably 15 to 100 grams per hectare.
[0093] The beneficial effects of this invention are as follows:
[0094] 1. This invention uses compounds with different mechanisms of action in insecticides and acaricides, mixed in a specific ratio, to achieve synergistic effects. This can delay the development of pesticide resistance in pests and improve the control effect on resistant populations. It shows a significant synergistic effect in insecticides and acaricides, and improves the control effect of single active ingredients in the composition on pests. At the same time, the synergistic effect of the combination of this invention is not linearly correlated with that of a single agent.
[0095] 2. The dosage of the composition of the present invention used in insecticidal and acaricidal applications is significantly lower than that of a single compound in the composition, thereby reducing usage costs and environmental pollution. Detailed Implementation
[0096] The following embodiments are intended to enable those skilled in the art to more fully understand the present invention, but are not intended to limit the invention to the scope of the embodiments described.
[0097] Compound source and quality analysis:
[0098] Compound I was synthesized in the laboratory, while the other compounds were obtained by extracting and purifying the reagents themselves after purchasing them from the laboratory.
[0099] Compound I: Chiral HPLC analysis showed that it was a mixture containing stereoisomers I-1 and I-2 in a ratio of 95.766%:3.247%. Stereoisomers I-3 and I-4 were below the detection limit.
[0100] 1 H NMR (400MHz, DMSO-d6) δ8.74-8.52(m,2H),7.82(d,J=6.1Hz,2H),7.59(dd,J=5.8,2.0Hz,2H),7.48(d,J=8 .4Hz,1H),4.48(p,J=7.2Hz,1H),4.43-4.25(m,2H),4.09-3.71(m,2H),2.37(s,3H),1.31(d,J=7.2Hz,3H).
[0101] Indoor bioactivity assay
[0102] Example 1.1 Determination of the synergistic effect of the composition containing compound I on diamondback moth larvae
[0103] Test subjects: Diamondback moth (Plutella xylostella) late 2nd instar and early 3rd instar larvae, a sensitive strain reared indoors.
[0104] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0105] Preparation of drug solution: According to different experimental needs, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a drug solution with a certain concentration gradient.
[0106] Experimental method: Select fresh cabbage leaves grown in greenhouse, punch holes in the cabbage leaves to make circular leaf discs with a diameter of 3cm, immerse them in the prepared solution for 10s, let them air dry naturally, and then place them in a petri dish with a diameter of 9cm containing filter paper. Inoculate healthy test insects neatly, 10-20 insects per treatment, with 3 replicates per treatment, and a blank control.
[0107] Based on his concept of synergistic toxicity, Bliss argued that the theoretical mortality rate P when insecticides and acaricides are mixed can be calculated using the following formula: P = P m +P n (1-P m )
[0108] P m The mortality rate (%) of the target at a concentration of m for the first active component; P n The mortality rate (%) of the target when the second active component is used at a concentration of n.
[0109] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, then the two active components are determined to have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect. The results are shown in Table 1.
[0110] Table 1. Synergistic effect of compound I in combination with four other agents, including pyriproxyfen, on diamondback moth larvae.
[0111] Example 1.2 Indoor activity assay of the composition containing compound I against diamondback moth larvae
[0112] Test subject: Diamondback moth (Plutella xylostella), late 2nd instar and early 3rd instar larvae.
[0113] Test conditions: Temperature: 24-26℃, Relative humidity: 60%, Light intensity: L:D = 14:10
[0114] Preparation method: Accurately weigh the test reagents using an electronic analytical balance, dissolve the two original drugs completely in an appropriate amount of solvent, and prepare the required concentration stock solution with water containing 0.1% Tween 80. Mix the two active ingredient stock solutions in a certain proportion to prepare a mixed solution, and dilute them according to the experimental design dosage to prepare a series of drug solutions with a certain concentration gradient.
[0115] Experimental method: First, select fresh cabbage leaves grown in greenhouse. Use a punch to make circular leaf discs with a diameter of 3cm. According to the experimental design, soak the cabbage leaves in the prepared solution for 10 seconds in order from low to high dose. After air drying, place them in a petri dish with a diameter of 9cm with filter paper. Inoculate healthy test insects neatly, 10-20 insects per treatment, with 3 replicates per treatment. A blank control is also set up.
[0116] The treated test materials were placed in an observation room, where the temperature, humidity, and light could be adjusted as needed. After 72 hours, the number of dead and live insects was investigated. The corrected mortality rate was calculated using the Abbott formula. Statistical analysis was performed using SPSS data processing software to determine the toxicity regression equations and LC-12 values for each single test agent and different mixtures. 50 The values and 95% confidence limits were determined, and the co-toxicity coefficients of each ratio were calculated using the Sun YP method to evaluate the effects of mixing. The experimental results are shown in Table 2.
[0117] Table 2. Results of indoor combined toxicity assays of compound I with four other agents, including pyriproxyfen, against diamondback moth.
[0118] The results showed that the co-toxicity coefficients of compound I with pyriproxyfen, lufenuron, thiamethoxam, and methoxyfenozide were all greater than 120, indicating that compound I had a synergistic effect with pyriproxyfen, lufenuron, thiamethoxam, and methoxyfenozide.
[0119] Example 2.1 Determination of the synergistic effect of the composition containing compound I on western flower thrips nymphs
[0120] Test subject: Western flower thrips (Frankliniella occidentalis) nymphs, a strain that has been raised indoors year-round.
[0121] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0122] Drug solution preparation: According to different experimental needs, the test samples (different ratio compositions and raw materials of the present invention) are accurately weighed using an electronic analytical balance. The raw materials are dissolved in acetone and diluted with the experimental design dosage to form drug solutions with a certain concentration gradient.
[0123] Experimental method: 0.5 mL of the prepared acetone solution was added to a glass tube, and the glass tube was repeatedly rolled until the acetone solution was completely evaporated. Cabbage leaves were immersed in the corresponding concentration of the solution for 10 seconds, then air-dried, and then placed in a glass tube. 20-30 western flower thrips larvae were inoculated into the glass tube. Each treatment was repeated three times. After treatment, the leaves were observed in a constant temperature observation room. The number of live and dead larvae was investigated after 72 hours, and the mortality rate was calculated. The results are shown in Table 3.
[0124] Table 3. Synergistic effect of compound I in combination with flonicamid and trifluralin on western flower thrips larvae.
[0125] Example 2.2 Determination of the synergistic effect of the composition containing compound I on western flower thrips larvae
[0126] Test subject: Western flower thrips (Frankliniella occidentalis), 2nd instar nymphs, an indoor strain that is kept year-round.
[0127] Preparation of drug solution: According to different experimental needs, the test samples are accurately weighed using an electronic analytical balance, the original drug is dissolved in acetone, and then diluted according to the experimental design dosage to form a series of drug solutions with a certain concentration gradient (the composition of this invention).
[0128] Experimental Method: 0.5 mL of the prepared acetone solution was added to a glass tube. The glass tube was repeatedly rolled on a flat table until the acetone solution completely evaporated. Cabbage leaves were immersed in the corresponding concentration of the solution for 10 seconds, then air-dried and placed in the glass tube. 20-30 western flower thrips larvae were inoculated into each glass tube. Each treatment was repeated three times. The number of dead and live thrips was counted after 72 hours. The corrected mortality rate was calculated using the Abbott formula. Statistical analysis was performed using SPSS software to determine the toxicity regression equations and LC-12 values for each tested single agent and each mixture with different ratios. 50 The values and 95% confidence limits were used to calculate the co-toxicity coefficients of each ratio using the Sun YP method to evaluate the effects of mixing. The results are shown in Table 4.
[0129] Table 4. Synergistic effect of compound I in combination with flonicamid and trifluralin on western flower thrips larvae.
[0130] The results showed that the co-toxicity coefficients of compound I with flonicamid and trifluoropyrimidine were all greater than 120, indicating that compound I had a synergistic effect with flonicamid and trifluoropyrimidine.
[0131] Example 3.1 Determination of the synergistic effect of the composition containing compound I on diamondback moth larvae
[0132] Test subjects: Diamondback moth (Plutella xylostella) late 2nd instar and early 3rd instar larvae, a sensitive strain reared indoors.
[0133] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0134] Preparation of drug solution: According to different experimental needs, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a drug solution with a certain concentration gradient.
[0135] Experimental method: Select fresh cabbage leaves grown in greenhouse, punch holes in the cabbage leaves to make circular leaf discs with a diameter of 3cm, immerse them in the prepared solution for 10s, let them air dry naturally, and then place them in a petri dish with a diameter of 9cm containing filter paper. Inoculate healthy test insects neatly, 10-20 insects per treatment, with 3 replicates per treatment, and a blank control.
[0136] Based on his concept of synergistic toxicity, Bliss argued that the theoretical mortality rate P when insecticides and acaricides are mixed can be calculated using the following formula: P = P m +P n (1-P m )
[0137] P m The mortality rate (%) of the target at a concentration of m for the first active component; P n The mortality rate (%) of the target when the second active component is used at a concentration of n.
[0138] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, then the two active components are determined to have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect. The results are shown in Table 5.
[0139] Table 5. Synergistic effect of compound I in combination with chlorantraniliprole and bromocyanamide on diamondback moth larvae.
[0140] Example 3.2 Indoor activity determination of the composition containing compound I against diamondback moth
[0141] Test subject: Diamondback moth (Plutella xylostella), late 2nd instar and early 3rd instar larvae, a sensitive strain raised indoors.
[0142] Test conditions: Temperature: 24-26℃, Relative humidity: 60%, Light intensity: L:D = 14:10
[0143] Preparation method: Accurately weigh the test reagents using an electronic analytical balance, dissolve the two original drugs completely in an appropriate amount of solvent, and prepare the required concentration stock solution with water containing 0.1% Tween 80. Mix the two active ingredient stock solutions in a certain proportion to prepare a mixed solution, and dilute them according to the experimental design dosage to prepare a series of drug solutions with a certain concentration gradient.
[0144] Experimental method: First, select fresh cabbage leaves grown in greenhouse. Use a punch to make circular leaf discs with a diameter of 3cm. According to the experimental design, soak the cabbage leaves in the prepared solution for 10 seconds in order from low to high dose. After air drying, place them in a petri dish with a diameter of 9cm with filter paper. Inoculate healthy test insects neatly. 10 insects per treatment, 3 replicates per treatment, and a blank control is set up.
[0145] The treated test materials were placed in an observation room, where temperature, humidity, and light could be adjusted as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using SPSS data processing software to determine the toxicity regression equations and LC-12 values for each single test agent and each mixture with different ratios. 50 The values and 95% confidence limits were used to calculate the co-toxicity coefficients of each ratio using the Sun YP method to evaluate the effects of mixing. The experimental results are shown in Table 6.
[0146] Table 6. Results of indoor combined toxicity assays of Compound I with chlorantraniliprole and bromocyanamide against diamondback moth.
[0147] The results showed that the co-toxicity coefficients of compound I with chlorantraniliprole and broflanilide were all greater than 120, indicating that compound I has a synergistic effect with chlorantraniliprole and broflanilide.
[0148] Example 4.1 Determination of the synergistic effect of the composition containing compound I on diamondback moth larvae
[0149] Test subject: Diamondback moth (Plutella xylostella), late 2nd instar and early 3rd instar larvae, a sensitive strain raised indoors.
[0150] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0151] Preparation of drug solution: According to different experimental needs, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a drug solution with a certain concentration gradient.
[0152] Experimental method: Select fresh cabbage leaves grown in greenhouse, punch holes in the cabbage leaves to make circular leaf discs with a diameter of 3cm, immerse them in the prepared solution for 10s, let them air dry naturally, and then place them in a petri dish with a diameter of 9cm containing filter paper. Inoculate healthy test insects neatly, 10-20 insects per treatment, with 3 replicates per treatment, and a blank control.
[0153] Based on his concept of synergistic toxicity, Bliss argued that the theoretical mortality rate P when insecticides and acaricides are mixed can be calculated using the following formula: P = P m +P n (1-P m )
[0154] P m The mortality rate (%) of the target at a concentration of m for the first active component; P n The mortality rate (%) of the target when the second active component is used at a concentration of n.
[0155] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, then the two active components are determined to have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect. The results are shown in Table 7.
[0156] Table 7. Synergistic effect of compound I in combination with avermectin on diamondback moth larvae.
[0157] Example 4.2 Indoor activity determination of the composition containing compound I against diamondback moth
[0158] Test subject: Diamondback moth (Plutella xylostella), late 2nd instar and early 3rd instar, a sensitive strain raised indoors.
[0159] Test conditions: Temperature: 24-26℃, Relative humidity: 60%, Light intensity: L:D = 14:10
[0160] Preparation method: Accurately weigh the test reagents using an electronic analytical balance, dissolve the two original drugs completely in an appropriate amount of solvent, and prepare the required concentration stock solution with water containing 0.1% Tween 80. Mix the two active ingredient stock solutions in a certain proportion to prepare a mixed solution, and dilute them according to the experimental design dosage to prepare a series of drug solutions with a certain concentration gradient.
[0161] Experimental method: First, select fresh cabbage leaves grown in greenhouse. Use a punch to make circular leaf discs with a diameter of 3cm. According to the experimental design, soak the cabbage leaves in the prepared solution for 10 seconds in order from low to high dose. After air drying, place them in a petri dish with a diameter of 9cm with filter paper. Inoculate healthy test insects neatly, 10-20 insects per treatment, with 3 replicates per treatment. A blank control is also set up.
[0162] The treated test materials were placed in an observation room, where temperature, humidity, and light could be adjusted as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using SPSS data processing software to determine the toxicity regression equations and LC-12 values for each single test agent and each mixture with different ratios. 50 The values and 95% confidence limits were determined, and the co-toxicity coefficients of each ratio were calculated using the Sun YP method to evaluate the effects of mixing. The experimental results are shown in Table 8.
[0163] Table 8. Results of indoor combined toxicity assay of compound I and avermectin against diamondback moth.
[0164] The results showed that the co-toxicity coefficients of compound I and avermectin were both greater than 120, indicating that compound I and avermectin have a synergistic effect.
[0165] Example 5.1 Determination of the synergistic effect of the composition containing compound I on the spider mite *Tetranychus carmine*.
[0166] Test subject: Tetranychus cinnabarinus, adult mite, sensitive strain kept indoors.
[0167] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0168] Preparation of drug solution: According to different experimental needs, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a drug solution with a certain concentration gradient.
[0169] Experimental method: The activity of the plant spray method against adult Tetranychus carinata was determined. First, 40-60 adult Tetranychus carinata of uniform size were transferred to a common bean seedling (leaving one true leaf) at the stage of unfolding the first pair of true leaves. After the adults stabilized, the population was counted. Then, the test material was treated with the pesticide solution using the Airbrush method, 1.5 mL per plant, with a blank control included.
[0170] After natural air drying, the treated test materials were placed in an observation room. The temperature, humidity, and light in the observation room could be adjusted as needed. After 72 hours, the number of live mites was investigated, and the mortality rate was calculated. The Bliss method was used for evaluation, which is one of the classic methods for evaluating the effects of mixtures. Based on his concept of synergistic toxicity, Bliss believed that the theoretical mortality rate P when insecticides and acaricides are mixed can be calculated using the following formula: P = P m +P n (1-P m )
[0171] P m The mortality rate (%) of the target at a concentration of m for the first active component; P n The mortality rate (%) of the target when the second active component is used at a concentration of n.
[0172] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, then the two active components are determined to have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect. The results are shown in Table 9.
[0173] Table 9. Synergistic effect of compound I in combination with avermectin on adult Tetranychus carmine.
[0174] Example 5.2 Indoor activity assay of the composition containing compound I against Tetranychus carmineus.
[0175] The synergistic effect data above show that the composition of compound I of the present invention mixed with three agents, including triazole tin, has a significant synergistic effect on adult Tetranychus cinnabarinus. Further LC-LC analysis was performed on the composition of compound I and triazole tin, propargite, and difenourea. 50 Value and co-toxicity coefficient were determined.
[0176] Test target: Adult Tetranychus cinnabarinus, a sensitive strain kept indoors.
[0177] Preparation of drug solution: According to different test requirements, the test samples are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a series of drug solutions with a certain concentration gradient (the composition of this invention).
[0178] Experimental Methods: The activity of the pesticide against adult Tetranychus carmineus was determined using a spray method. First, adult Tetranychus carmineus of uniform size were transferred to bean seedlings at the first true leaf unfolding stage (leaving one true leaf). After the adults stabilized, the population was counted. Then, the pesticide solution was sprayed evenly using the Airbrush method, from low to high doses, at a rate of 1.5 mL per plant. Each treatment was repeated three times, with a blank control included.
[0179] The treated test materials were placed in an observation room, where temperature, humidity, and light could be adjusted as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using SPSS data processing software to determine the toxicity regression equations and LC-12 values for each single test agent and each mixture with different ratios. 50 The values and 95% confidence limits were used to calculate the co-toxicity coefficients of each ratio using the Sun YP method to evaluate the effects of mixing. The results are shown in Table 10.
[0180] Table 10 Results of indoor combined toxicity assay of compound I and avermectin against Tetranychus carmine.
[0181] The results showed that the co-toxicity coefficient of compound I and avermectin was greater than 120, indicating that compound I and avermectin have a synergistic effect.
[0182] Example 6.1 Determination of the synergistic effect of the composition containing compound I on western flower thrips nymphs
[0183] Test subject: Western flower thrips nymphs, an indoor strain that is raised year-round.
[0184] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0185] Drug solution preparation: According to different experimental needs, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with the experimental design dosage to form a drug solution with a certain concentration gradient.
[0186] Experimental method: 0.5 mL of the prepared acetone solution was added to a glass tube (1 cm inner diameter, 10 cm length), and the glass tube was repeatedly rolled until the acetone solution was completely evaporated. Cabbage leaves were immersed in the corresponding concentration of the solution for 15 seconds, then air-dried, and then placed in the glass tube. 20-30 western flower thrips larvae were inoculated into the glass tube. Each treatment was repeated four times. After treatment, the leaves were observed in a constant temperature observation room. The number of live larvae was investigated after 72 hours, and the mortality rate was calculated. The results are shown in Table 11.
[0187] Table 11. Synergistic effect of compound I in combination with ethyl spinosad on western flower thrips larvae.
[0188] Example 6.2 Indoor activity determination of the composition containing compound I against western flower thrips
[0189] Test subject: Western flower thrips Frankliniella occidentalis, 2nd instar nymphs, an indoor strain that is kept year-round.
[0190] Preparation of drug solution: According to different experimental needs, the test samples are accurately weighed using an electronic analytical balance, the original drug is dissolved in acetone, and then diluted according to the experimental design dosage to form a series of drug solutions with a certain concentration gradient (the composition of this invention).
[0191] Experimental method: Add 0.5 mL of the prepared acetone solution to a glass tube (1 cm inner diameter, 10 cm length), and roll the glass tube repeatedly until the acetone solution evaporates completely. Immerse cabbage leaves in the corresponding concentration of the solution for 15 seconds, then air dry them, and then place them in a glass tube. Inoculate 20-30 western flower thrips larvae into the glass tube. Each treatment is repeated four times.
[0192] The treated test materials were placed in an observation room, where temperature, humidity, and light could be adjusted as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using SPSS data processing software to determine the toxicity regression equations and LC-12 values for each single test agent and each mixture with different ratios. 50 The values and 95% confidence limits were used to calculate the co-toxicity coefficients of each ratio using the Sun YP method to evaluate the effects of mixing. The results are shown in Table 12.
[0193] Table 12 Results of indoor combined toxicity assays of compound I with ethyl spinosad against western flower thrips.
[0194] The results showed that the co-toxicity coefficients of compound I with ethyl spinosad or abamectin were both greater than 120, indicating that compound I had a synergistic effect with ethyl spinosad or abamectin.
[0195] Example 7.1 Determination of the synergistic effect of the composition containing compound I on diamondback moth larvae
[0196] Test subject: Diamondback moth larvae, a sensitive strain reared indoors.
[0197] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0198] Preparation of drug solution: According to different experimental needs, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a drug solution with a certain concentration gradient.
[0199] Experimental method: Select fresh cabbage leaves grown in greenhouse, punch holes in the cabbage leaves to make circular leaf discs with a diameter of 3cm, immerse them in the prepared solution for 10s, let them air dry naturally, and then place them in a petri dish with a diameter of 9cm containing filter paper. Inoculate healthy test insects neatly, 10-20 insects per treatment, with 3 replicates per treatment, and a blank control.
[0200] Based on his concept of synergistic toxicity, Bliss argued that the theoretical mortality rate P when insecticides and acaricides are mixed can be calculated using the following formula: P = P m +Pn (1-P m )
[0201] P m The mortality rate (%) of the target at a concentration of m for the first active component; P n The mortality rate (%) of the target when the second active component is used at a concentration of n.
[0202] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, then the two active components are determined to have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect. The results are shown in Table 13.
[0203] Table 13. Synergistic effect determination of compound I in combination with two other agents, including cypermethrin, on diamondback moth larvae.
[0204] Example 7.2 Indoor activity assay of the composition containing compound I against diamondback moth larvae
[0205] Test subject: Diamondback moth (Plutella xylostella), late 2nd instar and early 3rd instar.
[0206] Test conditions: Temperature: 24-26℃, Relative humidity: 60%, Light intensity: L:D = 14:10
[0207] Preparation method: Accurately weigh the test reagents using an electronic analytical balance, dissolve the two original drugs completely in an appropriate amount of solvent, and prepare the required concentration stock solution with water containing 0.1% Tween 80. Mix the two active ingredient stock solutions in a certain proportion to prepare a mixed solution, and dilute them according to the experimental design dosage to prepare a series of drug solutions with a certain concentration gradient.
[0208] Experimental method: First, select fresh cabbage leaves grown in greenhouse. Use a punch to make circular leaf discs with a diameter of 3cm. According to the experimental design, soak the cabbage leaves in the prepared solution for 10 seconds in order from low to high dose. After air drying, place them in a petri dish with a diameter of 9cm with filter paper. Inoculate healthy test insects neatly. 10 insects per treatment, 3 replicates per treatment, and a blank control is set up.
[0209] The treated test materials were placed in an observation room, where the temperature, humidity, and light could be adjusted as needed. After 72 hours, the number of dead and live insects was investigated. The corrected mortality rate was calculated using the Abbott formula. Statistical analysis was performed using SPSS data processing software to determine the toxicity regression equations and LC-12 values for each single test agent and different mixtures. 50 The values and 95% confidence limits were used to calculate the co-toxicity coefficients of each ratio using the Sun YP method to evaluate the effects of mixing. The experimental results are shown in Table 14.
[0210] Table 14 Results of indoor combined toxicity assay of compound I and cypermethrin against diamondback moth.
[0211] The results showed that the co-toxicity coefficients of compound I with cypermethrin and indoxacarb were all greater than 120, indicating that compound I and abamectin have a synergistic effect.
[0212] Example 8.1 Determination of the synergistic effect of the composition containing compound I on the spider mite *Tetranychus cinnabarinus*.
[0213] Test subject: Tetranychus cinnabarinus, adult mite, sensitive strain kept indoors.
[0214] Test conditions: Temperature: 24-26℃, relative humidity: 60%, light intensity: L:D = 14:10.
[0215] Preparation of drug solution: According to different experimental needs, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a drug solution with a certain concentration gradient.
[0216] Experimental method: The activity of the mites against adult Tetranychus carinata was determined by spraying. First, 40-90 adult Tetranychus carinata of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding the first pair of true leaves. After the adults stabilized, the population was counted. Then, the test material was treated with the mites using the Airbrush method, 1.5 mL per plant. A blank control was set up.
[0217] After natural air drying, the treated test materials were placed in an observation room. The temperature, humidity, and light in the observation room could be adjusted as needed. After 72 hours, the number of live mites was investigated, and the mortality rate was calculated. The Bliss method was used for evaluation, a classic method for evaluating the effects of mixtures. Based on his concept of independent combined action, Bliss believed that the theoretical mortality rate P of a mixture of insecticides and acaricides could be calculated using the following formula: P = P m +P n (1-P m )
[0218] P m The mortality rate (%) of the target at a concentration of m for the first active component; P n The mortality rate (%) of the target when the second active component is used at a concentration of n.
[0219] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, then the two active components are determined to have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect. The results are shown in Table 15.
[0220] Table 15. Synergistic effect of compound I with five other agents, including etoxazole, on adult Tetranychus cinnabarinus.
[0221] As shown in the table above, compound I, when combined with etoxazole, spirodiclofen, propargite, bifenazate, and benzimidazole, has a significant synergistic effect on adult Tetranychus cinnabarinus.
[0222] Example 8.2 Indoor activity assay of the composition containing compound I against Tetranychus carmineus.
[0223] The synergistic effect data above show that the composition of compound I of the present invention mixed with three agents, including triazole tin, has a significant synergistic effect on adult Tetranychus cinnabarinus. Further LC-LC analysis was performed on the composition of compound I and triazole tin, propargite, and difenourea. 50 Value and co-toxicity coefficient were determined.
[0224] Test target: Adult Tetranychus cinnabarinus, a sensitive strain kept indoors.
[0225] Preparation of drug solution: According to different test requirements, the test samples are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a series of drug solutions with a certain concentration gradient (the composition of this invention).
[0226] Experimental Methods: The activity of the pesticide against adult Tetranychus carmineus was determined by spraying. First, adult Tetranychus carmineus of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding their first pair of true leaves. After the adults stabilized, the population was counted. Then, the pesticide solution was sprayed evenly using the Airbrush method, from low to high doses, at a rate of 1.5 mL per plant. Each treatment was repeated three times, with a blank control included.
[0227] The treated test materials were placed in an observation room, where temperature, humidity, and light could be adjusted as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using SPSS data processing software to determine the toxicity regression equations and LC-12 values for each single test agent and each mixture with different ratios. 50 The values and 95% confidence limits were determined, and the co-toxicity coefficients of each ratio were calculated using the Sun YP method to evaluate the effects of mixing. The experimental results are shown in Table 16.
[0228] Table 16 shows the results of indoor combined toxicity assays of Compound I with five other agents, including etoxazole, against *Tetranychus cinnabarinus*.
[0229] The results showed that the co-toxicity coefficient of compound I with etoxazole, spirodiclofen, propargite, bifenazate, and benzimidazole was greater than 120, indicating that compound I had a synergistic effect with etoxazole, spirodiclofen, propargite, bifenazate, and benzimidazole.
Claims
1. An insecticidal and miticidal composition, characterized by comprising, The composition contains active component A and active component B, the weight ratio between active component A and active component B is 1:100-100:1; the active component B is selected from one or more of the following: bionic juvenile hormone, chitin biosynthesis inhibitor affecting CHS1, chitin biosynthesis inhibitor type 1, ecdysone receptor agonist, competitive modulator of nicotinic acetylcholine receptors, Ryanodine receptor modulator, allosteric modulator of nicotinic acetylcholine receptors, allosteric modulator of glutamate-gated chloride channels, sodium channel modulator, voltage-dependent sodium channel blocker, inhibitor affecting chitin synthase 1 mite growth, mitochondrial ATP synthase inhibitor, mitochondrial electron transport complex (III) inhibitor, mitochondrial electron transport complex (I) inhibitor, acetyl-CoA carboxylase inhibitor, mitochondrial electron transport complex (II) inhibitor, trifluoromethylthioether acaricide and other insecticide / acaricide.
2. The insecticidal and miticidal composition according to claim 1, wherein The weight ratio between the active component A and the active component B is 1 :99 to 99:1, preferably 1 :80 to 80:1 ; and / or the bionomic juvenile hormone mimic is selected from one or more of methoprene, hydroprene, kinoprene, phoxim, and pyriproxyfen; and / or the chitin biosynthesis inhibitor affecting CHS1 is selected from one or more of diflubenzuron, flucycloxuron, hydroprene, flufenoxuron, and chlorfluazuron; and / or the chitin biosynthesis inhibitor type 1 is selected from one or more of thiacloprid and / or clothianidin; and / or the ecdysone receptor agonist is selected from one or more of chromafenozide, halofenozide, methoxyfenozide, and tebufenozide; and / or the nicotinic acetylcholine receptor competitive modulator is selected from one or more of nitenpyram, thiamethoxam, acetamiprid, dinotefuran, clothianidin, nitenpyram, thiacloprid, chloropyrifos, flonicamid, nuprid, sulfoxaflor, nicotine, sulfoxaflor, flupyradifurone, triflumuron, diacloden, and flupentiofene; and / or the ryanodine receptor modulator is selected from one or more of flubrocydamate, teflubenzuron, cyromazine, tetrahydrolindle, chlorfenapyr, chlorantraniliprole, and cyantraniliprole; and / or the nicotinic acetylcholine receptor allosteric modulator is selected from one or more of spinosad and / or spinosyn; and / or the glutamate-gated chloride channel allosteric modulator is selected from one or more of abamectin, emamectin benzoate, lepimectin, and milbemectin; and / or the sodium channel modulators class is selected from cypermethrin, lambda-cyhalothrin, fenpropathrin, fenvalerate, flucythrinate, flumethrin, beta-cyfluthrin, cyfluthrin, bifenthrin, deltamethrin, acrinathrin, alpha-cypermethrin, bioresmethrin, cyhalothrin, permethrin, fluvalinate, allethrin, bioallethrin, cycloprothrin, gamma-cyhalothrin, theta-cypermethrin, zeta-cypermethrin, cyphenothrin, empenthrin, esfenvalerate, imiprothrin, meperfluthrin, metofluthrin, dimefluthrin, prallethrin, phenothrin, resmethrin, bioresmethrin, cismethrin, tefluthrin, tetramethrin, tetramethylfluthrin, tralomethrin, beta-cypermethrin, ethofenprox, transfluthrin, esdépalléthrine, barthrin, bioethanomethrin, brofenvalerate, brofluthrinate, bromethrin, butethrin,one or more of chlorempenthrin, cyclethrin, cyhalothrin, lambda-cyhalothrin, dimethrin, d-fanshiluquebingjuzhi, fenfluthrin, fenpirithrin, esfenvalerate, furamethrin, imiprothrin, japothrins, kadethrin, methothrin, pentmethrin, biopermethrin, proparthrin, resmethrin, terallethrin, tralocythrin, valerate, flufenprox, halfenprox, sulfoxime, thiofluoximate, flumethrin, furethrin, heptafluthrin, momfluorothrin, transpermethrin, profluthrin, pyresmethrin, protrifenbute, silafluofen, DDT, and methoxychlor; and / or the voltage-dependent sodium channel blocker is selected from one or more of indoxacarb and / or metaflumizone; and / or the chitin synthesis inhibitor affecting mite growth is selected from one or more of clofentezine, flucycloxuron, hexythiazox, and etoxazole; and / or the mitochondrial ATP synthase inhibitor is selected from one or more of diafenthiuron, azocyclotin, cyhexatin, fenbutatin-oxide, propargite, and clofentezine; and / or the mitochondrial electron transport complex (III) inhibitor is selected from one or more of hydramethylnone, acequinocyl, bifenazate, and bifenazate; and / or the mitochondrial electron transport complex (I) inhibitor is selected from one or more of quinalphos, diafenthiuron, pyridaben, fenbutatin-oxide, acequinocyl, and rotenone; and / or the acetyl-CoA carboxylase inhibitor is selected from one or more of spirodiclofen, spiromesifen, methylobarbital, and spirotetramat; and / or the mitochondrial electron transport complex (II) inhibitor is selected from one or more of cyenopyrafen, ethyl tetrazanoate, cyflumetofen, and pyraziflumid; and / or the trifluoroethyl sulfide acaricide is selected from one or more of bentioflumin, bisulflufen, flufensulfone, sulfiflumin, and flupentiofeno; and / or other insecticidal acaricides are selected from one or more of azadirachtin, dry ice, boric acid, sulfonyl fluoride, benzoylurea, pyrimithione, sodium sulfadimethoxine, amitraz, and veratridine.
3. The insecticidal and miticidal composition according to claim 2, wherein The active component B is selected from one or more of pyriproxyfen, lufenuron, thiamethoxam and methoxyfenozide.
4. The insecticidal and miticidal composition according to claim 3, wherein The active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from pyridine; the weight ratio of the two active components is 1:50-30:1, preferably 1:30-30:1; Alternatively, active component A is selected from compound I, compound II or their stereoisomers, and active component B is selected from lufenuron; the weight ratio of the two active components is 1:50-30:1, preferably 1:50-20:1; Alternatively, active component A is selected from compound I, compound II or their stereoisomers, and active component B is selected from thiamethoxam; the weight ratio of the two active components is 1:50-30:1, preferably 1:50-20:1; Alternatively, the active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from methoxyfenozide; the weight ratio of the two active components is 1:50-30:1, preferably 1:50-20:
1.
5. The insecticidal and miticidal composition according to claim 2, wherein The active component B is selected from one or more of imidacloprid, flonicamid, and trifluorophenylpyrimidine.
6. The insecticidal and miticidal composition according to claim 5, wherein The active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from imidacloprid; the weight ratio of the two active components is 1:30-30:
1. Alternatively, active component A is selected from compound I, compound II or their stereoisomers, and active component B is selected from flonicamid; the weight ratio of the two active components is 1:80-20:1, preferably 1:40-5:1; Alternatively, the active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from trifluorophenylpyrimidine; the weight ratio of the two active components is 1:80-20:1, preferably 1:50-20:
1.
7. The insecticidal and miticidal composition according to claim 2, wherein The active component B is selected from chlorantraniliprole and / or bromocyanamide.
8. The insecticidal and miticidal composition according to claim 7, wherein The active component A is compound I, compound II or their stereoisomers, and the active component B is selected from chlorantraniliprole; the weight ratio of the two active components is 1:80-80:1, preferably 1:20-20:1; Alternatively, the active component A is compound I, compound II or their stereoisomers, and the active component B is selected from bromocyanamide; the weight ratio of the two active components is 1:50-50:1, preferably 1:30-30:
1.
9. The insecticidal and miticidal composition according to claim 2, wherein The active component B is selected from ethyl spinosad and / or avermectin.
10. The insecticidal and miticidal composition according to claim 9, wherein The active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from ethyl spinosad; the weight ratio of the two active components is 1:80-30:1, preferably 1:30-30:1; Alternatively, the active component A is selected from compound I, compound II or their stereoisomers, and the active component B is selected from avermectin; the weight ratio of the two active components is 1:30-100:1, preferably 1:30-30:
1.
11. The insecticidal and miticidal composition according to claim 2, wherein The active ingredient B is selected from cypermethrin and / or indoxacarb.
12. The insecticidal and miticidal composition according to claim 11, wherein said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from cypermethrin, the weight ratio of the two active components is 1:80-40:1, preferably 1:80-30:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from indoxacarb; the weight ratio of the two active components is 1:40-30:
1.
13. The insecticidal and miticidal composition according to claim 2, wherein said active component B is selected from one or more of ethiprole, veraceine, pyridaben, chinomethionat, bifenazate, spirodiclofen, ethyridifenconid and fenbutatin-oxide.
14. The insecticidal and miticidal composition according to claim 13, wherein said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from ethiprole, the weight ratio of the two active components is 1:30-30:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from veraceine; the weight ratio of the two active components is 1:30-30:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from pyridaben; the weight ratio of the two active components is 1:30-30:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from chinomethionat or chinomethionat; the weight ratio of the two active components is 1:100-30:1, preferably 1:80-30:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from bifenazate; the weight ratio of the two active components is 1:80-30:1, preferably 1:30-30:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from spirodiclofen or spiromesifen; the weight ratio of the two active components is 1:30-30:1, preferably 1:25-4:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from ethyridifenconid; the weight ratio of the two active components is 1:30-30:1, preferably 1:20-20:1; or, said active component A is selected from compound I, compound II or its stereoisomers, said active component B is selected from fenbutatin-oxide; the weight ratio of the two active components is 1:40-20:
1.
15. The insecticidal and acaricidal composition according to any one of claims 1 to 14, wherein said composition is mixed with a carrier and any one of the auxiliary agents to form a preparation containing said composition, the cumulative content of the active components of the composition in the preparation is between 0.5wt% and 95wt%; preferably, the cumulative content of the active components in the preparation is between 1wt% and 85wt%.
16. Use of the insecticidal and acaricidal composition according to any one of claims 1-15 in the preparation of an insecticidal and acaricidal agent for controlling agricultural or urban sanitary pests.
17. Use according to claim 16, characterized in that, The prepared insecticidal and acaricidal agent is applied to the pests to be controlled or the medium where the pests grow in an effective dose.
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