Sterilization composition containing Tolprocarb

Through the combination technology of Tolprocarb and allylbenthiazole, an efficient bactericidal composition is formed, which solves the high drug cost and bacterial resistance of allylbenthiazole, and achieves significant prevention and treatment effects and cost reduction.

CN119791124APending Publication Date: 2025-04-11SHAANXI SUNGER ROAD BIO SCI
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Patent Information

Application Number
CN202411996758.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-31
Publication Date
2025-04-11

AI Technical Summary

Technical Problem

In the prior art, the drug cost of allylbenthiazole is relatively high, and it is difficult to effectively reduce the dosage and cost of drugs, and there is also the problem of bacterial resistance.

Method used

By combining Tolprocarb and allylbenthiazole in a ratio of 30:1-1:30, a bactericidal composition is formed, and auxiliary ingredients such as emulsifiers, dispersants, etc. are added on this basis to prepare a variety of dosage forms that are allowed to be used in agriculture.

Benefits of technology

The compound sterilization composition significantly enhances the prevention and treatment effect of rice blast and tomato grey mold, reduces the amount of agent used, reduces the cost, and effectively delays the generation of bacterial resistance and extends the service life of the agent.

✦ Generated by Eureka AI based on patent content.

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Abstract

According to the sterilization composition containing the Tolprocarb, the effective active ingredients of the composition comprise the Tolprocarb and probenazole, the mass ratio of the Tolprocarb to the probenazole is (30: 1)-(1: 30), preferably (10: 1)-(1: 10), and the weight percentage content of the effective active ingredients in the composition is 1%-90%. The composition can be prepared into various agriculturally allowable pesticide formulations, the prevention and treatment effect is remarkably improved compared with that of a single agent, the use amount of pesticide can be effectively reduced, the use frequency of the pesticide is reduced, the cost is reduced, and the generation of pesticide resistance of pathogenic bacteria can be delayed.
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Description

Technical Field

[0001] The invention relates to a bactericidal composition, which consists of a first active ingredient, Tolprocarb, a second active ingredient, allylbenzazole and an adjuvant, and belongs to the technical field of pesticide compounding. Background Art

[0002] Tolprocarb is a carbamate fungicide developed by Mitsui Chemicals, Ltd., Japan. It has a unique mechanism of action and is a melanin biosynthesis polyketide synthase (PKS) inhibitor (MBI-P). It inhibits melanin biosynthesis by regulating the synthesis of polyketide compounds and pentaketide cyclization. Tolprocarb has systemic activity and can effectively prevent and control rice blast, pear scab, peach anthracnose, and gray mold and sclerotinia of many fruit trees, vegetables and other crops.

[0003] Probenazole, also known as allylisothiazole, is a benzisothiazole plant disease resistance activator. It achieves disease prevention by stimulating the plant's own immune (resistance) response to diseases. From the physiological and biochemical aspects, allylisothiazole can significantly increase the activity of three defense enzymes, such as PAL, POD and PPO, and can greatly enhance the resistance of rice to rice blast. Probenazole can be used to prevent and control rice blast, bacterial leaf blight and grain rot, and is also used to prevent and control bacterial diseases on vegetables, such as bacterial rot of lettuce, black rot of cabbage, soft rot of Chinese cabbage, bacterial soft rot of green onion and leaf spot of cucumber. Compared with other chemical agents, the advantages of allylbenzazole are: ① It has no obvious effect on the normal growth and development of plants and is a stable and highly effective resistance inducer for the prevention and control of rice blast; ② It has no direct activity on pathogens, so it does not produce selection pressure and it is not easy for pathogens to develop resistance to it; ③ It has no direct or indirect effect on non-pathogenic bacteria, which is beneficial to protecting beneficial microbial populations.

[0004] The cost of using allylbenzazole is relatively high. Considering the product performance and price factors, the research and development of compound products of allylbenzazole has become an important solution. Compound products can improve the prevention and control effect, reduce the amount of medicine used, reduce costs, further increase the market share of the agent and extend the service life of the agent. Summary of the invention

[0005] The object of the present invention is to provide a reasonable compound fungicide composition, which can achieve synergistic effect through reasonable compounding, has good fungicide effect, low drug cost and is safe for crops.

[0006] In order to achieve the above object, the present invention adopts the following technical scheme:

[0007] The invention provides a bactericidal composition containing Tolprocarb. The active ingredients of the composition include Tolprocarb and allylbenzazole, and the weight ratio of the two active ingredients is 30:1-1:30, preferably 10:1-1:10.

[0008] Calculated by mass percentage, the sum of the contents of Tolprocarb and allylbenzazole is 1% to 90% of the total weight of the composition.

[0009] The bactericidal composition containing Tolprocarb of the present invention can be prepared into various dosage forms allowed for use in agriculture according to methods known to those skilled in the art.

[0010] The various application formulations prepared from the pesticide composition of the invention include, in addition to effective active ingredients, various auxiliary ingredients that are permitted and acceptable in different pesticide formulations.

[0011] The auxiliary ingredients include, but are not limited to, emulsifiers, dispersants, wetting agents, solvents, antifreeze agents, defoamers, thickeners, disintegrants, synergists, preservatives and fillers, etc., which are all commonly used or permitted ingredients in pesticide formulations and are not particularly limited. The specific ingredients and amounts are determined through experiments based on the formulation requirements.

[0012] The emulsifier may be any emulsifier known in the field of pesticide formulations, and may be one or more of phenylethylphenol polyoxyethylene polyoxypropylene ether, alkylaryl polyoxyethylene polyoxypropylene ether, fatty acid polyoxyethylene ether, fatty alcohol polyoxyethylene ether, glycerol laurate polyoxyethylene ether, styrylphenol polyoxyethylene ether, castor oil polyoxyethylene ether, alkylphenol polyoxypropylene polyoxyethylene ether, styrylphenyl polyoxyethylene ether, alkylphenol polyoxyethylene ether, sorbitan fatty acid ester polyoxyethylene ether, fatty alcohol polyoxyethylene ether sulfonate, alkylphenol polyoxyethylene formaldehyde condensate, calcium dodecyl sulfonate, alkylphenol polyoxyethylene ether succinic acid monoester sulfonate, alkylphenol polyoxyethylene phosphate, and alkylphenol polyoxyethylene ether sulfonated succinate.

[0013] The dispersant may be any of various dispersants known in the field of pesticide formulations, and may be one or more of alkylphenol polyoxyethylene ether phosphate, alkylphenol polyoxyethylene ether sulfate, phenethylphenol polyoxyethylene ether phosphate, polyoxyethylene polyoxypropylene ether block copolymer, sodium lignin sulfonate, sodium methylene dinaphthalene sulfonate (dispersant NNO), calcium lignin sulfonate, polycarboxylate, sodium methylene bisnaphthalene sulfonate, sodium methylene bismethylnaphthalene sulfonate, polyvinyl pyrrolidone, alkylamido taurate, sodium salt of alkylnaphthalene sulfonic acid polycondensate, and sodium methylene bisnaphthalene sulfonate formaldehyde condensate.

[0014] The wetting agent can be various wetting agents known in the field of pesticide formulations, and can be one or more of sodium alkylnaphthalene sulfonate, sodium dodecyl sulfate, sodium secondary alkyl sulfate, sodium dodecylbenzene sulfonate, fatty alcohol polyglycol ether sulfate, fatty alcohol polyoxyethylene ether, nonylphenol polyoxyethylene ether, sorbitan fatty acid ester polyoxyethylene ether, alkylnaphthalene formaldehyde condensate, alkylnaphthalene sulfonate and other wetting agents.

[0015] The solvent may be any solvent known in the field of pesticide formulations, and may be one or more of water, methanol, ethanol, N-methylpyrrolidone, N,N-dimethylformamide, N,N-dimethylacetamide, tetrahydrofurfuryl alcohol, toluene, xylene, dimethyl sulfoxide, tetrahydrofuran, cyclohexanone, n-butanol, isopropanol, solvent oil No. 100, No. 150, No. 180, and No. 200.

[0016] The antifreeze agent may be any antifreeze agent known in the field of pesticide formulations, and the antifreeze agent may be one or more of ethylene glycol, propylene glycol, glycerol, diethylene glycol, urea, and inorganic salts.

[0017] The defoamer may be any defoamer known in the field of pesticide formulations, and may be one or more of silicone compounds, epoxy soybean oil, emulsified silicone oil, and fatty alcohol.

[0018] The thickener may be any thickener known in the field of pesticide formulations, and may be one or more of xanthan gum, polyvinyl alcohol, sodium alginate, gum arabic, and magnesium aluminum silicate.

[0019] The disintegrant may be any disintegrant known in the field of pesticide formulations, and may be one or more of ammonium sulfate, sodium carboxymethyl starch, urea, low-substituted hydroxypropyl cellulose, cross-linked sodium carboxymethyl cellulose, cross-linked polyvinylpyrrolidone, sodium alginate, sodium bicarbonate, and sodium chloride.

[0020] The carrier can be various carriers known in the field of pesticide formulation, and can be one or more of glucose, white carbon black, kaolin, diatomaceous earth, light calcium carbonate, heavy calcium carbonate, attapulgite, soluble starch, urea, maltose, sucrose, citric acid, potassium carbonate, sodium carbonate, and anhydrous sodium sulfate.

[0021] The preservative may be any preservative known in the field of pesticide formulations, and the preservative may be one or more of kasone, sodium benzoate, benzoic acid, potassium sorbate, and formaldehyde.

[0022] The deionized water is industrial deionized water.

[0023] The production processes of various application formulations of the pesticide composition belong to existing known technologies and will not be described in detail here.

[0024] Beneficial effects achieved by the present invention:

[0025] 1. Tolprocarb and allylbenzazole have a significant synergistic effect when mixed in a certain ratio;

[0026] 2. Compared with single agent, compound preparation has significantly improved field control effect, which can effectively reduce the amount of pesticide used, reduce costs and protect the environment;

[0027] 3. The effective active ingredients Tolprocarb and allylbenzazole of the present invention have different mechanisms of action. After mixing, they can effectively delay the development of bacterial resistance and extend the service life of the agent. DETAILED DESCRIPTION

[0028] The technical solution of the present invention is described below in conjunction with specific embodiments, but the specific protection scope of the present invention includes but is not limited to the following specific embodiments.

[0029] 1. Indoor toxicity test of Tolprocarb and allylbenzazole against rice blast pathogen

[0030] The test method adopted the potting method.

[0031] Inoculation materials: 20 rice seeds of rice blast susceptible varieties were sown in each pot, and 10 rice seedlings at the 3-leaf 1-heart stage with consistent growth were selected as rice blast inoculation materials.

[0032] Test strains: The rice blast pathogen stored in a 4°C refrigerator was transferred to PSA medium and cultured in a 25°C incubator to activate it. After two transfers to produce spores, the spores were washed with sterile water and filtered through 4 layers of gauze to make a 1×10 5 spores / mL suspension for later use.

[0033] Experimental treatment: The test agent was prepared into 5 concentration gradients, and the clear water treatment was used as the blank control. Each treatment was repeated 4 times. A three-dimensional crop sprayer was used to spray the agent on each treatment, and then dried naturally in the shade. After 24 hours, the rice blast fungus spore suspension was sprayed on the rice, placed in an artificial climate culture room at (27±1)℃ and relative humidity>95% for 24 hours, and then moved to a temperature of 25-26℃, 12h light and dark alternation, and relative humidity of 85%-90% for routine management. After 7 days, according to the leaf disease situation, when the blank control disease rate reached more than 50%, the leaves of each treatment were investigated and graded, and the control effect was calculated.

[0034] The rice blast survey classification standards are as follows:

[0035] Grade 0, no lesions;

[0036] Level 1, brown spots appear;

[0037] Level 3: Typical spindle-shaped lesions appear, and the lesion area accounts for less than 5% of the entire leaf area;

[0038] Level 5: typical lesions, some of which are connected into pieces, accounting for 5% to 25% of the leaf area;

[0039] Level 7, typical lesions, lesions are connected into pieces, occupying 26% to 50% of the leaf area;

[0040] Level 9: typical lesions, covering more than 50% of the leaf area or all the leaves are dead.

[0041]

[0042] Calculate the toxicity regression equation and EC according to the protective effect 50 The combined effect of the two drugs was evaluated by the Sun Yunpei co-toxicity coefficient method (CTC). The co-toxicity coefficient of the compound drug CTC ≥ 120 showed synergistic effect; CTC ≤ 80 showed antagonistic effect; 80 < CTC < 120 showed additive effect.

[0043]

[0044] Theoretical toxicity index TTI = ∑ (ATI of a drug × the percentage of the active ingredient of the drug in the mixture)

[0045]

[0046] Table 1 Determination of the combined action of Tolprocarb and allylbenzazole on rice blast fungus

[0047]

[0048] As shown in Table 1, when Tolprocarb and allylbenzazole were mixed in a ratio of 30:1 to 1:30, they showed a certain synergistic effect on rice blast fungus.

[0049] 2. Indoor toxicity test of Tolprocarb and allylbenzazole against Botrytis cinerea

[0050] The test method adopts the mycelium growth rate method.

[0051] Drug-containing culture medium: Prepare drug-containing plate PDA culture medium, prepare the test drug into 5 concentration gradients, use a pipette to draw the test drug solution of different concentration gradients and inject it into a sterile culture dish. The volume ratio of the drug and the culture medium is 1:9. Mix well to make drug-containing plate PDA culture medium. Repeat each treatment 3 times.

[0052] Experimental treatment: Use a puncher to punch the bacterial cake at the edge of the tomato gray mold colony after 3 days of culture, and put it upside down in the center of the drug-containing plate. Use the plate without drug as a control and culture it in a constant temperature box at 25℃. After 3 days, measure the colony diameter by the cross method, and calculate the inhibition rate of different drugs and different concentrations of drugs on the growth of pathogenic fungi, and calculate the EC of each drug. 50 The co-toxicity coefficient method (CTC) of Sun Yunpei method was used to evaluate the combined effect of the two drugs.

[0053] Table 2 Determination of the combined action of Tolprocarb and allylbenzazole on tomato gray mold

[0054]

[0055]

[0056] As shown in Table 2, Tolprocarb and allylbenzazole were mixed in a ratio of 30:1 to 1:30, which showed a certain synergistic effect on tomato gray mold.

[0057] In order to better illustrate the present invention, the present invention is further described below in conjunction with the formulation examples, and the percentages in the formulations are all weight percentages.

[0058] Preparation Example 1

[0059] Tolprocarb 10%, allylbenzazole 10%, sodium lignin sulfonate 5%, sodium alkyl sulfonate 3%, polyvinyl alcohol 3%, clay added to 100% by weight. The above raw materials are mixed evenly in a mixing tank, and 20% Tolprocarb allylbenzazole granules are prepared through extrusion, granulation, drying, screening and other steps.

[0060] Preparation Example 2

[0061] Tolprocarb 5%, allylbenzazole 15%, polycarboxylate T36 3.5%, sodium alkylnaphthalene sulfonate 4%, sodium dibutylnaphthalene sulfonate 4%, sodium dodecyl sulfate 2.5%, kaolin added to 100%. The above raw materials are mixed, ultrafine air flow pulverized, mixed, and granulated to prepare 20% Tolprocarb·allylbenzazole water dispersible granules.

[0062] Preparation Example 3

[0063] Tolprocarb 5%, allylbenzazole 15%, 5% of pulverized powder, 4% of polyoxyethylene polyoxypropylene ether block copolymer, 3% of sodium alkyl sulfate, 3% of carboxymethyl cellulose, 3% of potassium sorbate, 3% of butanol, and deionized water are added to 100% by weight. The above raw materials are mixed, dispersed at high speed shear for 30 minutes, and sand-milled to a particle size D90 of less than 10 μm to obtain a 20% Tolprocarb·allylbenzazole suspension.

[0064] Biological Example 1: Field efficacy test for controlling rice blast.

[0065] In 2024, field efficacy tests of Formulation Example 1, Formulation Example 2, and Formulation Example 3 for controlling rice blast were conducted. Plot area: 20m 2 Each treatment was repeated 3 times, and the water treatment was used as the blank control. The granules were applied by broadcasting, and the other preparations were sprayed by conventional method. After the blank control leaf blight occurred, the leaf blight was investigated, and the neck spike blight was investigated during the milky stage. The diagonal five-point sampling method was used, and 50 plants were selected at each point, for a total of 250 plants. For leaf blight, the sword leaf and two leaves below the sword leaf were investigated for each plant, and the disease index and control effect were calculated. The disease classification standard and calculation formula are as follows:

[0066] Leaf blight grading standards:

[0067] Level 0: no disease;

[0068] Level 1: There are less than 5 leaf spots, and the length is less than 1 cm;

[0069] Level 3: There are 6 to 10 lesions on the leaves, some of which are longer than 1 cm;

[0070] Level 5: There are 11 to 25 leaf spots, some of which are connected in a line, accounting for 10% to 25% of the leaf area;

[0071] Level 7: There are more than 26 lesions on the leaves, which are connected in a line and occupy 26% to 50% of the leaf area;

[0072] Level 9: The lesions are connected into pieces, occupying more than 50% of the leaf area or all the leaves are dead;

[0073] Grading standards for neck spike blight:

[0074] Level 0: no disease;

[0075] Level 1: less than 5% loss per ear (individual branches and stalks are diseased);

[0076] Level 3: 6% to 20% loss per ear (about 1 / 3 of the branches and stalks are diseased);

[0077] Level 5: 21% to 50% loss per ear (the neck or main axis of the ear is diseased, and the grains are half-shrunken);

[0078] Level 7: 51% to 70% loss per ear (the neck of the ear is diseased and most of the grains are shrunken);

[0079] Level 9: 71% to 100% loss per ear (the ear neck becomes diseased, resulting in white ears);

[0080] Calculation formula:

[0081]

[0082] Table 3 Results of field trials on controlling rice blast

[0083]

[0084]

[0085] As shown in Table 3, the combination of Tolprocarb and allylbenzazole can effectively control rice blast, and the control effect is better than that of a single agent, and there is no adverse effect on the target within the experimental medication range.

[0086] In summary, the present invention is a fungicide composition of Tolprocarb and allylbenzazole. After the two compounds are compounded, the synergistic effect on rice blast, tomato gray mold and the like is significant. Field efficacy tests show that no phytotoxicity occurs within the dosage range. The present invention has the characteristics of good rapid effect and long lasting effect, can effectively reduce costs and reduce environmental pollution. The invention and promotion of the compound preparation are of great significance to society.

Claims

1. A bactericidal composition containing Tolprocarb, characterized in that: The effective active ingredients of the bactericidal composition include Tolprocarb and allylbenzazole, and the mass ratio of Tolprocarb to allylbenzazole is 30:1-1:

30.

2. A bactericidal composition containing Tolprocarb according to claim 1, characterized in that: The mass ratio of the active ingredient Tolprocarb to allylbenzazole is 10:1-1:

10.

3. A bactericidal composition containing Tolprocarb according to claim 1, characterized in that: The active ingredients Tolprocarb and allylbenzazole account for 1% to 90% of the composition by weight.

4. A bactericidal composition containing Tolprocarb according to claim 1, characterized in that: The dosage form of the bactericidal composition is granules, suspensions and water-dispersible granules.

5. Use of the fungicidal composition containing Tolprocarb according to claim 1 for controlling plant pathogenic fungi.

6. The use according to claim 5, characterized in that: The use is: preventing and controlling rice blast, tomato leaf blight, tomato gray mold, vegetable soft rot, cucumber leaf spot, pear black spot, and peach anthracnose.