Amide derivative containing 3, 4-dichloroisothiazole as well as preparation method and application thereof

Abstract

The invention provides an amide derivative containing 3, 4-dichloroisothiazole as well as a preparation method and application thereof, and particularly relates to a derivative of which the chemical structural general formula is shown as a formula I: # imgabs0 #. The invention discloses the structural general formula and the synthesis method of the compound and application of the compound as a plant activator, an insecticide, a bactericide, an anti-plant virus agent and the plant activator. The invention also relates to application and a preparation method of the compound in preventing and treating insect pests, diseases and virus diseases of agricultural, forestry and horticultural plants in combination with agriculturally acceptable auxiliaries or synergists and commercial insecticides, bactericides, plant virus resisting agents, acaricides and plant immune activators.

Description

Technical Field

[0001] The technical scheme of the invention belongs to the field of pesticides, and specifically relates to an amide derivative containing 3,4-dichloroisothiazole, and a preparation method and use thereof. Background Art

[0002] As one of the important means of plant protection, pesticides play an extremely important role in solving the problem of pests and diseases and increasing the yield of grain crops. They are strategic materials related to national stability and economic development. However, with the extensive use of pesticides, problems such as resistance of pests and diseases, pesticide residues and environmental pollution have also arisen. Therefore, the creation of new pesticides with high efficiency, low toxicity, low residue and environmental friendliness has become a top priority in research (Shao Xusheng et al. World Pesticides, 2020, 42(04):16-24). Therefore, "green ecological pesticides" plant activators with the characteristics of broad spectrum, low toxicity, no resistance risk and hysteresis and long lasting effect, and synergistic or synergistic effects when mixed with other fungicides have become an important direction for the creation of green pesticides. However, the current development of plant activators has problems such as few lead molecules, unclear mechanism of action research, and difficult targeted design.

[0003] Isotianil is a plant activator for the prevention and treatment of rice blast developed jointly by Bayer and Sumitomo Chemical (Himmler, et al. WO2004002968). Isothiazolamide compounds including Isotianil have enhanced plant induction activity in plants. When applied preventively or in the early stage of the disease, various biological and non-biological factors can activate the plant's own defensive resistance response, i.e., systemic induced resistance, and affect multiple links in the life history of pathogens, thereby enabling plants to produce a broad spectrum of self-protection against a variety of fungi, bacteria, insects and viruses; Isotianil can provide long-term residual efficacy and a smaller dosage of the active ingredient, which is suitable for inducing plant defense to prevent plants from being attacked by pathogenic fungi, bacteria, viruses and pests, and can be used to protect plants from the above-mentioned harmful organisms for a certain period of time after treatment. A series of 3,4-dichloroisothiazole carboxamide and formate derivatives designed by the applicant's research group in the early stage have better disease resistance inducing plants than isothiocyanate at low concentrations (Chen Xiaoyan et al. CN102942565A.2016-01-27). The present invention retains 3,4-dichloroisothiazole and designs and synthesizes a series of amide derivatives containing 3,4-dichloroisothiazole, which show good immune induction activity at lower concentrations and can be used as candidate molecules for plant activators. Summary of the invention

[0004] The technical problem to be solved by the present invention is to provide a method for synthesizing a new type of amide derivatives containing 3,4-dichloroisothiazole, provide biological activities of such compounds in regulating agricultural, horticultural, sanitary and forestry plant pests and plant pathogens and a method for determining the same, and provide applications of these compounds in the fields of agriculture, horticulture, forestry and sanitation.

[0005] The technical solution adopted by the present invention to solve the technical problem is: the chemical structure of an amide derivative containing 3,4-dichloroisothiazole having insecticidal, acaricidal, bactericidal, anti-plant virus activity, and plant disease resistance inducing activity in the agricultural, horticultural, and forestry fields is shown in I:

[0006] I:

[0007] Among them, R 1 , R 2 , R 3 Selected from: substituted alkyl, substituted alkenyl, hydrogen, substituted alkynyl, substituted cycloalkyl, substituted cycloalkenyl, substituted cycloalkynyl, substituted alkoxy, substituted alkenyloxy, substituted alkynyloxy, substituted phenyl, substituted heterocyclyl;

[0008] The heterocyclic group is selected from: furanyl, thienyl, imidazolyl, pyrazolyl, pyridyl, pyranyl, indolyl, pyrimidinyl, triazine, isoindolyl and other nitrogen- and / or sulfur-containing three-membered ring groups, four-membered ring groups, five-membered ring groups and six-membered ring groups.

[0009] R 3 Also selected from: Li, Na, K,

[0010] n is selected from 1, 3, and 4;

[0011] The above substituents are preferably:

[0012] R 1 Selected from: 1-methylethyl, 1-methylpropyl, hydrogen, 2-(methylthio)ethyl, imidazole-4-methyl, 2-methylpropyl, indole-3-methyl, 3-methoxy-3-oxopropyl, methyl, benzyl, cyclohexylmethyl, methyl, benzyl, p-phenolmethyl, 2-amino-2-oxoethyl, hydroxymethyl, ethoxy, 3-guanidinopropyl, 4-aminobutyl, carboxymethyl; R 2 is selected from hydrogen, methyl; R 3 Selected from hydrogen, sodium, methyl, ethyl, propyl, butyl, isopropyl; n is selected from 1, 3, 4.

[0013] The synthetic route of the amide derivative I containing 3,4-dichloroisothiazole of the present invention is as follows:

[0014]

[0015] The synthesis method of the amide derivative I containing 3,4-dichloroisothiazole of the present invention comprises the following steps:

[0016] A. Preparation of Compound I:

[0017] At room temperature, 1 equivalent of carbamate hydrochloride 2 is added to dichloromethane, and then 2 equivalents of triethylamine are added. After stirring at room temperature for 1 minute, 1.1 equivalents of compound 1 are added, and the mixture is stirred at room temperature for 6 hours. 20 ml of sodium bicarbonate solution is added to quench the mixture, and the aqueous phase is extracted with dichloromethane. The organic phases are combined, and the organic phases are washed three times with saturated brine and dried over anhydrous sodium sulfate. The solvent is removed under reduced pressure, and the residue is purified by 200-300 mesh silica gel column chromatography, and the eluent is ethyl acetate / petroleum ether to obtain an amide derivative I containing 3,4-dichloroisothiazole; the carbamate hydrochloride is selected from: 2-amino-3-phenylpropionic acid methyl ester hydrochloride, 1-aminocyclopropane-1-carboxylic acid ethyl ester hydrochloride, cycloleucine methyl ester hydrochloride, 2-aminoisobutyric acid methyl ester hydrochloride, 2-amino-3-cyclohexylpropionic acid methyl ester hydrochloride, 1-aminocyclohexanecarboxylic acid methyl ester hydrochloride, L-valine methyl ester hydrochloride, L-isoleucine methyl ester hydrochloride, L-methionine methyl ester hydrochloride, L-histidine methyl ester dihydrochloride, L-leucine tert-butyl ester hydrochloride, L-tryptophan methyl ester hydrochloride, L-glutamic acid dimethyl ester hydrochloride, glycine methyl ester hydrochloride, L-alanine methyl ester hydrochloride, L-phenylalanine methyl ester hydrochloride, L-tyrosine methyl ester hydrochloride, L-asparagine methyl ester hydrochloride, L-serine methyl ester hydrochloride, L-threonine methyl ester hydrochloride, L-arginine methyl ester hydrochloride, L-lysine methyl ester hydrochloride, L-aspartic acid methyl ester hydrochloride, L-proline methyl ester hydrochloride, D-3-aminobutyric acid, β-aminobutyric acid.

[0018] B. Uses of amide derivatives I containing 3,4-dichloroisothiazole:

[0019] The invention provides use of an amide derivative I containing 3,4-dichloroisothiazole in preparing a fungicide. The fungi are: tomato early blight pathogen, whose Latin name is Alternaria solani; cucumber gray mold pathogen, whose Latin name is Botrytis cinerea; peanut brown spot pathogen, whose Latin name is Cercospora arachidicola; graminearum fusarium, whose Latin name is Fusarium graminearum; apple ring spot pathogen, whose Latin name is Physalosporapiricola; rice sheath blight pathogen, whose Latin name is Rhizoctonia solani; and rapeseed sclerotinia pathogen, whose Latin name is Sclerotinia sclerotiorum.

[0020] The invention provides use of an amide derivative I containing 3,4-dichloroisothiazole in preparing a plant immune activator for preventing and controlling fungal diseases. The fungi are diseases: tomato early blight, whose Latin name is Alternaria solani, cucumber gray mold, whose Latin name is Botrytis cinerea, peanut brown spot, whose Latin name is Cercosporaarachidicola, graminearum fusarium, whose Latin name is Fusarium graminearum, apple ring rot, whose Latin name is Physalospora piricola, rice sheath blight, whose Latin name is Rhizoctonia solani, and rapeseed sclerotinia, whose Latin name is Sclerotinia sclerotiorum.

[0021] The present invention provides use of an amide derivative I containing 3,4-dichloroisothiazole in preparing an anti-tobacco mosaic virus agent.

[0022] The present invention provides use of an amide derivative I containing 3,4-dichloroisothiazole in preparing a plant activator for inducing tobacco to resist tobacco mosaic virus.

[0023] The present invention provides use of an amide derivative I containing 3,4-dichloroisothiazole in preparing insecticides and acaricides.

[0024] The present invention provides use of an amide derivative I containing 3,4-dichloroisothiazole in preventing and controlling insect pests in agriculture, forestry and horticultural plants.

[0025] The present invention provides an amide derivative I containing 3,4-dichloroisothiazole, which is suitable for preventing and controlling insect pests and pathogens of agricultural, forestry and horticultural plants and inducing plants to produce defense capabilities against plant insect pests and pathogens. The above-mentioned pesticide composition includes an agricultural fungicide composition, an agricultural insecticide composition, an agricultural anti-plant virus composition, and an agricultural plant activator composition. The composition contains the amide derivative of 3,4-dichloroisothiazole as an active ingredient; the composition contains 0.1% to 99.9% by weight of the active ingredient, 99.9% to 0.1% by weight of a solid or liquid adjuvant, and 0 to 25% by weight of a surfactant.

[0026] C. Compositions and uses thereof of amide derivatives I containing 3,4-dichloroisothiazole:

[0027] The amide derivative I containing 3,4-dichloroisothiazole and commercial pesticides are used together to form an agricultural composition; the commercial pesticides are selected from: one or more of insecticides, fungicides, anti-plant virus agents, miticides, and plant activators. The composition contains the amide derivative I of 3,4-dichloroisothiazole and other commercial insecticides, fungicides, anti-plant virus agents, miticides, and plant activators as active ingredients; the content of the active ingredient in the composition is 1%:99% to 99%:1% by weight, and the composite composition contains 1% to 99% by weight of active ingredients, 99% to 1% by weight of solid or liquid adjuvants, and 0 to 25% by weight of surfactants. The specific combination is as follows:

[0028] The amide derivative I containing 3,4-dichloroisothiazole is combined with any one or two of the insecticides to form an insecticidal composition for controlling agricultural, forestry and horticultural plant pests;

[0029] The insecticide is selected from the group consisting of methoprene, dimethoate, acetamiprid, avermectin, mibemycin, avermectin, spinosad, tefluthrin, cypermethrin, cypermethrin, cypermethrin, deltamethrin, cypermethrin, β-cypermethrin, λ-cypermethrin, cypermethrin, allethrin, bifenthrin, permethrin, ether cypermethrin, flumethrin, cypermethrin, imidacloprid, nitenpyram, chlorthiazolin, thiacloprid, thiamethoxam, clothianidin, dinotefuran, clothianidin, datenam, diflubenzuron, diflubenzuron, flufenoxuron, acetamiprid, lufenuron, chlorpyrifos, flufenuron, polyflubenzuron, flufenuron , bisbenzenefluanid, chlorfluazuron, anthracene, bistrifluanid, furanfenozide, fenfenozide, chlorfenapyr, methoxyfenozide, chlorfenapyr, dichlorvos, quinalphos, pyridazine, leafhopper powder, carbaryl, pirimicarb, mefenamic acid, isoprocarb, cartap, fenbutyl, leaf flying powder, carbaryl, cartap, bromocriptine, hexythiazox, fenpyroximate, pyridabenzan, clofenazine, fenpyroximate, pyrimidine, pyridabenzan, clofenazine, fenpyroximate, pyrimidine, pyridabenzan, spirocyclon, spirocyclon, spirocyclon, triazotin, buprofezin, insecticide single, insecticide double, chlorantraniliprole, tetrachlorantraniliprole, flubendiamide, flucyram, cyanamide, butene flubendiamide, tolfenpyrad, bromofenapyr, pyrazinone, etoxazole, cypermethrin, pyridabenzan, pyriproxyfen, emamectin, pyrimidine;

[0030] The mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the insecticide composition is 1%-90%; preferably, the mass percentage of the amide derivative I containing 3,4-dichloroisothiazole to the insecticide is 1%:99% to 99%:1%;

[0031] The dosage form of the insecticide composition is selected from the group consisting of seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granule, fine granule, soluble concentrate, poisonous grain, block poison bait, granular poison bait, sheet poison bait, concentrated poison bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot fog, cold fog, aerosol, solid / liquid mixed agent, liquid / liquid mixed agent, solid / solid mixed agent, lacquer, microgranule, tracking powder, oil suspension, oil dispersible powder, concentrated glue, pouring agent, seed coating agent, smear, film-forming oil agent, ultra-low volume liquid agent, steam release agent;

[0032] The plant pests controlled by the insecticide composition are selected from: fall armyworm, red spider, East Asian migratory locust, cloud-spotted locust, Chinese rice locust, Japanese yellow-spine locust, single-spined mole cricket, oriental mole cricket, rice thrips, tobacco thrips, greenhouse thrips, rice tube thrips, wheat tube thrips, greenhouse whitefly, Bemisia tabaci, black-tailed leafhopper, green leafhopper, cotton leafhopper, spotted wax cicada, brown planthopper, white-backed planthopper, gray planthopper, sugarcane flat-horned planthopper, cotton aphid, wheat aphid, wheat long-tube aphid, peach aphid, sorghum aphid, radish aphid, cotton scale, mulberry shield scale, arrow-pointed shield scale, pear round scale, white wax insect, red wax scale, Korean ball-hard scale , pear web bug, banana web bug, fine-horned flower bug, tiny flower bug, needle-edged bug, rice spider bug, rice brown bug, rice black bug, rice green bug, green stink bug, alfalfa stink bug, middle black stink bug, big lacewings, beautiful lacewings, Chinese lacewings, grain moth, clothes moth, yellow thorn moth, brown thorn moth, flat thorn moth, wheat moth, cotton pink bollworm, sweet potato wheat moth, diamondback moth, peach borer, soybean borer, peach borer, apple top leaf roller, brown-banded long leaf roller, quasi-small yellow leaf roller, striped stem borer, bean pod borer, corn borer, yellow stem borer, cabbage borer, rice leaf roller, striped stem borer, cotton leaf roller, peach borer, sticky insect, twill Noctuidae, rice borer, cotton bridgeworm, beet armyworm, stem borer, cotton bollworm, Dingdian diamond drill, small cutworm, large cutworm, yellow cutworm, thief moth, gypsy moth, sweet potato hawkmoth, bean hawkmoth, straight-striped rice hesperid, hidden grain hesperid, citrus swallowtail, jade-belt swallowtail, cabbage butterfly, ramie red admiral, ramie yellow admiral, bean sedge, Venus carabid, wrinkled sheath carabid, wheat ear carabid, ditch wireworm, fine-breasted wireworm, grain spot beetle, black skin beetle, citrus small borax, golden-margin borax, yellow mealworm, black mealworm, red flour beetle, mixed flour beetle, copper green exotic beetle, dark beetle, North China giant Black-gilled scarab beetle, mulberry longhorn beetle, star longhorn beetle, orange brown longhorn beetle, peach-necked longhorn beetle, big monkey leafworm, small monkey leafworm, yellow melon beetle, yellow-striped flea beetle, mung bean weevil, pea weevil, broad bean weevil, corn weevil, rice weevil, wheat sawfly, pear sawfly, yellow-banded ichneumon wasp, white-star ichneumon wasp of sticky insect, hanging cocoon ichneumon wasp of cotton bollworm, black-spotted warty ichneumon wasp of stem borer, mosquito, fly, horsefly, red wheat midge, yellow wheat midge, rice gall midge, citrus fruit fly, melon fruit fly, wheat leaf gray leafminer, American spotted leafminer, bean stalk black leafminer, wheat stalk fly, seed fly, onion fly, radish fly, skirt chasing fly, corn borer fly, and sticky insect;

[0033] The plants controlled by the insecticide composition are selected from the group consisting of: rice, wheat, barley, oats, corn, sorghum, sweet potato, potato, cassava, soybean, snow pea, broad bean, pea, mung bean, adzuki bean, cotton, sericulture, peanut, rapeseed, sesame, sunflower, beet, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rapeseed, onion, garlic, watermelon, melon, cantaloupe, papaya, apple, citrus and peach, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, and bonsai.

[0034] The amide derivative I containing 3,4-dichloroisothiazole is combined with any one or two of the fungicides to form a fungicide composition for preventing and controlling agricultural, forestry and horticultural plant diseases;

[0035] The fungicide is selected from the group consisting of benzothiadiazole, thiazolamide, thiazolamide, DL-β-aminobutyric acid, isothiopyrad, viravirin, anthofen, ningnanmycin or salicylic acid, cymoxanil, thiram, zinc thiram, mancozeb, ethyl phosphine aluminum, methyl thiophanate, chlorothalonil, dichlorobenzene, procymidone, fenpropidin, methyl thiophanate, thiophanate, metalaxyl, flumorph, dimethomorph, high-efficiency metalaxyl, high-efficiency bensulfuron, dichlorocyanamide, sulfaquinoxaline, sulfaquinoxaline, thiofluanid, chlorothalonil, cyproconazole, cyprodinil, cyfluanid, cyprodinil, cyanamide, cyprodinil ... Azopyraclostrobin, Fluoxathiapiprolin, Fluoxathiapiprolin, Isopropyltrifloxacin, Fluoxathiapiprolin, Fluoxathiapiprolin, Fluoxathiapiprolin, Dimethomorph, Zoxystrobin, Ethioprolin, Iprodione, Azoxystrobin, Dimethomorph, Fluoxathiapiprolin, Dimethomorph, Ethiostrobin ... azole, cyproconazole, difenoconazole, diniconazole, high-efficiency diniconazole, fluepiconazole, nitrobenazole, fluquinconazole, flusilazole, flutriafol, hexaconazole, imidazole, cyproconazole, metconazole, myclobutanil, penconazole, propiconazole, prothioconazole, silyfloxacin, tebuconazole, tetrafluconazole, triadimenol, trichlorfonazole, bifenthrin, thiabendazole, wheat spike, imazalil, high-efficiency imazalil, prochloraz, Flubaccon, cyazofamid, imidacloprid, oxacloprid, oxacloprid, oxacloprid, oxacloprid, oxacloprid, oxathiapiprolin, oxadixyl, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, oxathiapiprolin, Bensulfuron, furamide, carbendazim, benomyl, methyl thiophanate, triadimefon, ethiminol sulfonate, dimethoate, ethiminol, captan, foltan, vinyl sclerotin, fluchloric acid sclerotin, sclerotin, thiophanate-methyl, chlorothalonil, rice blast, rice blast, leaf chloranil, pentachloronitrobenzene, propineb, fosetyl-aluminum, sulfur, Bordeaux mixture, copper sulfate, copper oxychloride, cuprous oxide, copper hydroxide, bensulfuron, pencuron, pyraclostrobin, tetrachlorophthalide, pyroquilone, spiroxafil, tricyclazole, thiamethoxam, polypyrimidine, biguanide salt, biguanide octylamine, chloranil, benzylsulfuron, toluenesulfuron, indole ester, sodium sulfensulfuron, quinoline, allyl thiazole, bronopol, iodomethane, metamethylenetetramine, dazomethanil, dichloroisopropyl ether, thiathion, fensulfuron, chloranil,Oxamyl, sulfuryl fluoride, dichloropropylene, dichloroisonicotinic acid, allylisothiazole;

[0036] The total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the bactericidal composition is 1%-90%; the ratio of the amide derivative I containing 3,4-dichloroisothiazole to the bactericide is 1%:99% to 99%:1% by mass;

[0037] The dosage form of the bactericidal composition is selected from the group consisting of seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granule, fine granule, soluble concentrate, poisonous grain, block poison bait, granular poison bait, sheet poison bait, concentrated poison bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot mist, cold mist, aerosol, solid / liquid mixed agent, liquid / liquid mixed agent, solid / solid mixed agent, lacquer, microgranule, tracking powder, oil suspension, oil dispersible powder, concentrated glue, pouring agent, seed coating agent, smear, film-forming oil agent, ultra-low volume liquid agent, steam release agent;

[0038] The plant diseases controlled by the bactericidal composition are selected from: rice seedling rot, tomato root rot, potato late blight, tobacco black shank, millet powdery mildew, grape downy mildew, lettuce downy mildew, cucumber downy mildew, cucumber anthracnose;

[0039] The plants suitable for the fungicidal composition are selected from the group consisting of: rice, wheat, barley, oats, corn, sorghum, sweet potato, potato, cassava, soybean, snow pea, broad bean, pea, mung bean, adzuki bean, cotton, sericulture, peanut, rapeseed, sesame, sunflower, beet, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rapeseed, onion, garlic, watermelon, melon, cantaloupe, papaya, apple, citrus and peach, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, and bonsai.

[0040] The amide derivative I containing 3,4-dichloroisothiazole is combined with any one or two of the antiviral agents to form an antiviral composition for preventing and controlling viral diseases of agricultural, forestry and horticultural plants;

[0041] The antiviral agent is selected from: benzothiadiazole, thiazolamide, isothiazolamide DL-β-aminobutyric acid, 2,6-dichloroisonicotinic acid, N-cyanomethyl-2-chloroisonicotinamide, allylisothiazole, ribavirin, anthofin, ningnanmycin, methiothiazolamide or salicylic acid, pyrimidine, dichloroisonicotinic acid, allylisothiazole, Jinggangmycin, guanidine hydrochloride;

[0042] The total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the antiviral composition is 1%-90%; preferably, the mass percentage of the amide derivative I containing 3,4-dichloroisothiazole to the anti-plant virus agent is 1%:99% to 99%:1%;

[0043] The dosage form of the antiviral composition is selected from the group consisting of seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granule, fine granule, soluble concentrate, poisonous grain, block poison bait, granular poison bait, sheet poison bait, concentrated poison bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot mist, cold mist, aerosol, solid / liquid mixed agent, liquid / liquid mixed agent, solid / solid mixed agent, lacquer, microgranule, tracking powder, oil suspension, oil dispersible powder, concentrated glue, pouring agent, seed coating agent, smear, film-forming oil agent, ultra-low volume liquid agent, steam release agent;

[0044] The virus diseases controlled by the antiviral composition are selected from: rice dwarf disease, yellow dwarf disease, stripe leaf blight, tomato fern leaf virus disease, pepper mosaic virus disease, tobacco vein necrosis virus disease, corn dwarf mosaic virus, cauliflower mosaic virus, citrus virus disease, Jianlan orchid leaf virus, and Jianlan ringspot virus;

[0045] The plants for prevention and treatment of the antiviral composition are selected from the group consisting of rice, wheat, barley, oats, corn, sorghum, sweet potato, potato, cassava, soybean, snow pea, broad bean, pea, mung bean, adzuki bean, cotton, sericulture, peanut, rapeseed, sesame, sunflower, beet, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rapeseed, onion, garlic, watermelon, melon, cantaloupe, papaya, apple, citrus and peach, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, and bonsai.

[0046] The amide derivative I containing 3,4-dichloroisothiazole is combined with any one or two of the acaricides to form an acaricidal composition for preventing and controlling acaricide damage in agriculture, forestry and horticultural plants;

[0047] The acaricide is selected from the group consisting of dichlorvos, heptylphos, cypermethrin, dibromophos, pyrimidophos, chlormethoxam, ethion, acaricide, phosalone, methyl pyrimidophos, quinalphos, aphidox, chlormethoxam, phosmet, flumethrin, bifenthrin, cyhalothrin, cyhalothrin, cyhalothrin, cyhalothrin, cyhalothrin, cyhalothrin, cyhalothrin, bifenthrin, fenthiocarb, butanone, oxamyl, cypermethrin, long-lasting cypermethrin, benomyl, chlormethrin ... Wei, butyralidone, cypermethrin, benzyl benzoate, bromocriptine, cyfluthrin, acequinoxaline, flumioxon, flufenoxuron, liuyangmycin, cypermethrin, thuringin, miticide, liuyangmycin, avermectin, doramectin, eprinomectin, ivermectin, selamectin, moxidectin, pyrethrin, nicotine, matrine, azadirachtin, rotenone, cypermethrin, pyraclostrobin, cypermethrin ...

[0048] The total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the acaricide composition is 1%-90%; the mass percentage of the amide derivative I containing 3,4-dichloroisothiazole to the acaricide is 1%:99% to 99%:1%;

[0049] The dosage form of the acaricide composition is selected from the group consisting of seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granule, fine granule, soluble concentrate, poisonous grain, block poison bait, granular poison bait, sheet poison bait, concentrated poison bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot fog, cold fog, aerosol, solid / liquid mixed agent, liquid / liquid mixed agent, solid / solid mixed agent, lacquer, microgranule, tracking powder, oil suspension, oil dispersible powder, concentrated glue, pouring agent, seed coating agent, smear, film-forming oil agent, ultra-low volume liquid agent, steam release agent;

[0050] The mite pests controlled by the acaricidal composition are selected from the group consisting of pests of Tetranychus, Tenebriophyidae, Furonematodes, Cynocephalus, Tetranychus, and Cynocephalus, and the pests are global agricultural pests, forestry pests, gardening pests, and hygiene pests;

[0051] The plants for the control of the acaricide composition are selected from the group consisting of rice, wheat, barley, oats, corn, sorghum, sweet potatoes, potatoes, cassava, soybeans, snow peas, broad beans, peas, mung beans, adzuki beans, cotton, sericulture, peanuts, rapeseed, sesame, sunflowers, sugar beets, sugar cane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomatoes, peppers, radishes, cucumbers, cabbages, celery, mustard tubers, sugar beets, rapeseed, onions, garlic, watermelons, melons, cantaloupes, papayas, apples, citrus and peach trees, tea, wild vegetables, bamboo shoots, hops, peppers, bananas, papayas, orchids, and bonsai.

[0052] The amide derivative I containing 3,4-dichloroisothiazole is combined with any one or two of the plant immune activators to form a plant immune activator composition for preventing and controlling agricultural, forestry and horticultural plant diseases;

[0053] The plant activator agent is selected from the group consisting of benzothiadiazole, isothiazolin, S-inducing agent, oligosaccharide chain protein, amino oligosaccharide, lentinan, fluazole activated ester, oligosaccharide, chitosan, fluothioate, DL-β-aminobutyric acid, 2,6-dichloroisonicotinic acid, N-cyanomethyl-2-chloroisonicotinamide, allylisothiazole, methylthiazolin, coronatine, salicylic acid, Jinggangmycin, hypersensitive protein, laminarin, pyraclostrobin, and allylisothiazole thiabendazole;

[0054] The total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the plant immune activator composition is 1%-90%; preferably, the ratio of the amide derivative I containing 3,4-dichloroisothiazole to the plant immune activator is 1%v99% to 99%:1% by mass;

[0055] The dosage form of the plant immune activator composition is selected from the group consisting of seed treatment emulsions, aqueous emulsions, microemulsions, suspoemulsions, capsule suspensions, water-soluble granules, fine granules, soluble concentrates, poisonous grains, block poison baits, granular poison baits, sheet poison baits, concentrated poison baits, slow-release blocks, electrostatic sprays, oil-in-water emulsions, smoke cans, smoke candles, smoke tubes, smoke sticks, smoke sheets, smoke pills, gasifiers, ointments, hot mists, cold mists, aerosols, solid / liquid mixed preparations, liquid / liquid mixed preparations, solid / solid mixed preparations, lacquers, microgranules, tracking powders, oil suspensions, oil-dispersible powders, concentrated glues, pouring agents, seed coatings, smears, film-forming oils, ultra-low volume liquids, and steam release agents;

[0056] The diseases controlled by the anti-plant immune activator composition are selected from: rice seedling rot, tomato root rot, potato late blight, tobacco black shank, millet powdery mildew, grape downy mildew, lettuce downy mildew, cucumber downy mildew, cucumber anthracnose, rice dwarf disease, yellow dwarf disease, stripe leaf blight, tomato fern leaf virus disease, pepper mosaic virus disease, tobacco vein necrosis virus disease, corn dwarf mosaic disease, cauliflower mosaic virus, citrus virus disease, Jianlan orchid leaf virus, and Jianlan ringspot virus;

[0057] The plants for which the plant immune activator composition is used to prevent and control are selected from: rice, wheat, barley, oats, corn, sorghum, sweet potato, potato, cassava, soybean, snow pea, broad bean, pea, mung bean, adzuki bean, cotton, sericulture, peanut, rapeseed, sesame, sunflower, beet, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rapeseed, onion, garlic, watermelon, melon, cantaloupe, papaya, apple, citrus and peach, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, bonsai.

[0058] The biological activity of the amide derivative I containing 3,4-dichloroisothiazole of the present invention is determined as follows:

[0059] Determination of fungicidal activity of the amide derivative I containing 3,4-dichloroisothiazole of the present invention:

[0060] The bactericidal or antibacterial activity of the amide derivative I containing 3,4-dichloroisothiazole of the present invention is determined by a bacterial growth rate determination method, which specifically comprises the following steps: 1.8 mg of a sample is dissolved in 2 drops of dimethyl sulfoxide, and then diluted to 500 μg / ml of the drug with an aqueous solution containing a certain amount of Tween 20 emulsifier, 1 ml of each test drug is aspirated into a culture dish under sterile conditions, and then 9 ml of PDA culture medium is added respectively, and after being shaken, a 50 μg / ml drug-containing plate is prepared, and a plate with 1 ml of sterilized water added is used as a blank control, and a plate with a diameter of 4 is used to measure the bactericidal or antibacterial activity of the amide derivative I containing 3,4-dichloroisothiazole ... Use a millimeter puncher to cut the bacterial disc along the outer edge of the hyphae, move it to the drug-containing plate, and place it in an equilateral triangle. Repeat each treatment 3 times, and place the culture dish in a constant temperature incubator at 24 degrees Celsius for cultivation. After the diameter of the control colony expands to 2-3 cm, investigate the expansion diameter of the bacterial disc of each treatment, calculate the average value, and calculate the relative inhibition rate by comparing with the blank control. The test strains are the species of most typical plant pathogens that actually occur in the field in my country's agricultural production. Their codes and names are as follows: As: Tomato early blight pathogen, its Latin name is: Alternaria solani, Bc: Cucumber gray mold, its Latin name is: Botrytis cinerea, Ca: Peanut brown spot fungus, its Latin name is: Cercospora arachidicola, Fg: Grainite Fusarium, its Latin name is: Fusarium graminearum, Pp: Apple ring rot fungus, its Latin name is: Physalospora piricola, Rc: Grainite Sclerotinia, its Latin name is: Rhizoctonia cerealis, Ss: Rapeseed Sclerotinia, its Latin name is: Sclerotinia sclerotiorum.

[0061] Determination of the in vivo immune-inducing activity of the amide derivative I containing 3,4-dichloroisothiazole of the present invention:

[0062] The immune induction activity of the amide derivative I containing 3,4-dichloroisothiazole of the present invention against Arabidopsis downy mildew is determined by a spore counting method, and the specific steps are as follows: 1.8 mg of the sample is dissolved in 2 drops of N,N-dimethylformamide, and then diluted to 100 micromol / L of the agent with an aqueous solution containing a certain amount of Tween 20 emulsifier. Arabidopsis (Col-0) seeds are sown in the soil of a growth chamber, and after growing for 2 weeks in a cycle of 16 hours of light (22 degrees Celsius) / 8 hours of darkness (20 degrees Celsius), 20 Arabidopsis seedlings are sprayed with 1 ml of a 100 micromol / L concentration of the agent; 0.2% DMF (N,N-dimethylformamide) without the test compound is used as a control. After 24 hours of chemical treatment, the seedlings with Arabidopsis downy mildew collected and separated are vortexed in sterile water, and then the spores in the water are counted with a hemacytometer to determine the number of spores, and the spores diluted to 5×10 4The Arabidopsis seedlings were inoculated with a spore solution of Peronospora thaliana at spores / ml. After inoculation, the seedlings were placed in an incubator at a temperature of 18 degrees Celsius and a humidity of 80-100% and observed for 7 days. To determine the number of spores, the collected seedlings were vortexed in sterile water and then counted with a hemocytometer and the relative inhibition rate was calculated compared with the control. Each treatment included three replicates.

[0063] The beneficial effects of the present invention are as follows: the amide derivative I containing 3,4-dichloroisothiazole is synthesized, and the antibacterial activity of the amide derivative I containing 3,4-dichloroisothiazole is screened and the activity of inducing plant resistance to fungal diseases, bacterial diseases and viral diseases is screened.

[0064] The present invention further specifically illustrates the synthesis, biological activity and application of the amide derivative I containing 3,4-dichloroisothiazole through specific preparation and biological activity determination examples. The examples are only used to specifically illustrate the present invention but not to limit the present invention. In particular, the biological activity is only an example and not to limit the present patent. The specific implementation method is as follows:

[0065] Example 1: Preparation of Compound I-14:

[0066] In a 100 ml single-necked round-bottom flask, glycine methyl ester hydrochloride (126.0 mg, 1.0 mmol) was dissolved in 20 ml of dichloromethane, and 2 equivalents of triethylamine (0.29 ml, 2.0 mmol) were added. After stirring at room temperature for 1 minute, 1.1 equivalents of 3,4-dichloroisothiazole-5-carbonyl chloride (0.16 ml, 1.1 mmol) were added. The mixture was stirred at room temperature for 6 hours, quenched by adding 20 ml of sodium bicarbonate solution, extracted three times with 20 ml of dichloromethane, the organic phases were combined, washed three times with 20 ml of saturated brine, and dried over anhydrous sodium sulfate. The solvent was removed under reduced pressure, and the residue was purified by 200-300 mesh silica gel column chromatography, the eluent was ethyl acetate / petroleum ether = 1:5 (volume ratio), to obtain 229 mg of light yellow solid I-14, the yield was 85%, the chemical structure and physicochemical parameters of the compound synthesized by the present invention are shown in Tables 1 and 2.

[0067] Example 2: Antibacterial activity test results of the amide derivative I of 3,4-dichloroisothiazole of the present invention:

[0068] The codes and names of the common plant pathogenic fungi tested by the present invention are as follows: As: Alternaria solani, Bc: Botrytis cinerea, Ca: Cercospora arachidicola, Fg: Fusarium graminearum, Pp: Physalospora piricola, Rs: Rhizoctonia solani, Ss: Sclerotinia sclerotiorum. These strains are very representative and can represent most of the species of pathogens occurring in the field during agricultural production.

[0069] The results of the bacterial growth rate method are shown in Table 3, which shows that at 50 μg / ml, methyl jasmonate (MeJA) and commercial plant activators BTH, ISO, and TDL were used as positive controls to carry out the biological activity determination of the new compound I. The results show that the compound synthesized by the present invention itself has no significant bactericidal activity against 7 pathogens under in vitro conditions, which is consistent with the characteristics that the plant activator itself has no in vitro activity or low in vitro activity.

[0070] Example 3: Determination of in vivo immune-inducing activity of the amide derivative I of 3,4-dichloroisothiazole of the present invention:

[0071] The bacteria used for the in vivo immune activity test of the present invention are Arabidopsis downy mildew. The test results are shown in Table 4. Table 4 shows that at 50 micromol / L, the induced disease resistance activity of all the compounds synthesized by the present invention is above 70%, which is more than 30% higher than the positive control compound ISO. Among them, the induced disease resistance activity of I-1, I-2, I-3, I-4, I-5, I-6, I-8, I-9, I-10, I-11, I-12, I-13, and I-14 to Arabidopsis downy mildew is above 85%, which is more than 45% higher than the 38% of the control drug ISO. The induced disease resistance activity of I-4, I-9, I-11, I-12, I-13, and I-14 to Arabidopsis downy mildew reaches 100%, which is higher than 38% and 26% of the positive control drugs ISO and MeJA, and is very close to the 99% of BTH in terms of value. The results of the test of reducing the concentration showed that at 10 μmol / L, the positive control ISO had only 13% of the induced disease resistance activity, almost losing its biological activity, while the induced disease resistance activity of compounds I-1, I-2, I-3, I-4, I-5, I-6, I-8, I-9, I-10, I-11, I-12, I-13, and I-14 against Arabidopsis thaliana downy mildew was above 45%, among which I-4 and I-14 had induced disease resistance activity of more than 90%, which was better than the positive control drug BTH. Based on the results of Example 3, it was found that the compounds of the present invention belong to plant activators; the characteristics of plant activators are that they have a broad spectrum of disease resistance activity, and the effects of the compounds of the present invention on plant pathogenic fungi, bacteria and viruses are comparable to their induced activity against Arabidopsis thaliana downy mildew, which are significantly higher than the positive control ISO.

[0072] Example 4: Application of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in the preparation of a pesticide composition:

[0073] The pesticide composition is prepared from the amide derivative I containing 3,4-dichloroisothiazole of the present invention, which contains the amide derivative I containing 3,4-dichloroisothiazole of the present invention as an active ingredient, the mass percentage of the active ingredient is 0.1% to 99.9%, the mass percentage of a solid or liquid adjuvant is 99.9% to 0.1%, and further contains an optional surfactant in an amount of 0 to 25% by mass.

[0074] Example 5: Application of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in the preparation of a pesticide compound composition:

[0075] The amide derivative I containing 3,4-dichloroisothiazole of the present invention can be compounded with other commercial pesticides, i.e., insecticides, miticides, fungicides, antiviral agents or plant activators to prepare a pesticide compound composition. The compound composition comprises the amide derivative I containing 3,4-dichloroisothiazole of the present invention and commercial pesticides, i.e., insecticides, miticides, fungicides, antiviral agents or plant activators as active ingredients. The ratio of the amide derivative I containing 3,4-dichloroisothiazole of the present invention to the other commercial pesticides, i.e., insecticides, miticides, fungicides, antiviral agents or plant activators is 1% by mass: 99% to 99%: 1% by mass, the mass percentage of the active ingredient is 0.1% to 99.9%, 99.9% to 0.1% by mass of a solid or liquid adjuvant, and optionally 0 to 25% by mass of a surfactant.

[0076] Example 6: Application of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in combination with a plant activator in controlling insect pests of agricultural, forestry and horticultural plants:

[0077] The amide derivative I containing 3,4-dichloroisothiazole of the present invention is combined with any one or two of commercial plant immune activators to form a plant immune activator composition for preventing and controlling agricultural, forestry and horticultural plant diseases;

[0078] The plant activator agent is selected from the group consisting of benzothiadiazole, isothiazolin, S-inducing agent, oligosaccharide chain protein, amino oligosaccharide, lentinan, fluazole activated ester, oligosaccharide, chitosan, fluothioate, DL-β-aminobutyric acid, 2,6-dichloroisonicotinic acid, N-cyanomethyl-2-chloroisonicotinamide, allylisothiazole, methylthiazolin, coronatine, salicylic acid, Jinggangmycin, hypersensitive protein, laminarin, pyraclostrobin, and allylisothiazole thiabendazole;

[0079] The total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the plant immune activator composition is 1%-90%; preferably, the mass percentage of the amide derivative I containing 3,4-dichloroisothiazole to the plant immune activator is 1%:99% to 99%:1%;

[0080] The dosage form of the plant immune activator composition is selected from the group consisting of seed treatment emulsions, aqueous emulsions, microemulsions, suspoemulsions, capsule suspensions, water-soluble granules, fine granules, soluble concentrates, poisonous grains, block poison baits, granular poison baits, sheet poison baits, concentrated poison baits, slow-release blocks, electrostatic sprays, oil-in-water emulsions, smoke cans, smoke candles, smoke tubes, smoke sticks, smoke sheets, smoke pills, gasifiers, ointments, hot mists, cold mists, aerosols, solid / liquid mixed preparations, liquid / liquid mixed preparations, solid / solid mixed preparations, lacquers, microgranules, tracking powders, oil suspensions, oil-dispersible powders, concentrated glues, pouring agents, seed coatings, smears, film-forming oils, ultra-low volume liquids, and steam release agents;

[0081] The diseases controlled by the anti-plant immune activator composition of the present invention are selected from: rice seedling rot, tomato root rot, potato late blight, tobacco black shank, millet powdery mildew, grape downy mildew, lettuce downy mildew, cucumber downy mildew, cucumber anthracnose, rice dwarf disease, yellow dwarf disease, stripe leaf blight, tomato fern leaf virus disease, pepper mosaic virus disease, tobacco vein necrosis virus disease, corn dwarf mosaic disease, cauliflower mosaic virus, citrus virus disease, Jianlan orchid leaf virus, and Jianlan ringspot virus;

[0082] The plants that the plant immune activator composition of the present invention is used to control are selected from: rice, wheat, barley, oats, corn, sorghum, sweet potato, potato, cassava, soybean, snow pea, broad bean, pea, mung bean, adzuki bean, cotton, sericulture, peanut, rape, sesame, sunflower, beet, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rape, onion, garlic, watermelon, melon, Hami melon, papaya, apple, citrus and peach, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, bonsai.

[0083] Example 7: Application of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in combination with an insecticide in controlling insect pests in agriculture, forestry and horticultural plants:

[0084] The amide derivative I containing 3,4-dichloroisothiazole of the present invention is combined with any one or two of commercial insecticides to form an insecticidal composition for preventing and controlling agricultural, forestry and horticultural plant pests. The commercial insecticide is selected from the group consisting of methoprene, dimethoate, acetamiprid, avermectin, mibemycin, avermectin, spinosad, tefluthrin, cypermethrin, high-efficiency cypermethrin, high-efficiency cypermethrin, tri-cyhalothrin, deltamethrin, cypermethrin, β-cypermethrin, λ-cypermethrin, dichlorophenoxyacetate, permethrin, allethrin, bifenthrin, permethrin, etherpermethrin, flumethrin, fluvalinate , imidacloprid, nitenpyram, chlorthiophene, thiacloprid, thiamethoxam, clothianidin, dimethoate, clothianidin, datenam, diflubenzuron, diflubenzuron, diflubenzuron, diflubenzuron, flufenoxuron, acetamiprid, lufenuron, chlorfenapyr, flufenoxuron, flufenoxuron, flufenoxuron, flufenoxuron, flufenoxuron, flufenoxuron, flufenoxuron, flufenoxuron, bistriflubenzuron, furanthinofen, fenfenoxadone, chlorfenoxadone, methoxyfenoxadone, chlorfenapyr ... , pymetrozine, spirodiclofen, spirothiocarb, spirothiocarb, triazotin, buprofezin, cypermethrin, dimethoate, chlorantraniliprole, tetrachlorvinphos, flubendiamide, flucyantraniliprole, cyantraniliprole, butene-fipronil, tolfenpyrad, chlorfenapyr, pyrazinone, etoxazole, cypermethrin, pyriproxyfen, pyriproxyfen, emamectin, and pyrimidineguanidine; the mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the insecticidal composition of the present invention is 1%-90%, and the ratio of the amide derivative I containing 3,4-dichloroisothiazole of the present invention to the aforementioned commercial insecticide is 1%:99% to 99%:1% by mass; the insecticidal composition The processed dosage form is selected from: seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granule, fine granule, soluble concentrate, poisonous grain, block poison bait, granular poison bait, sheet poison bait, concentrated poison bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot fog, cold fog, aerosol, solid / liquid mixed agent, liquid / liquid mixed agent, solid / solid mixed agent, lacquer, microgranule, tracking powder, oil suspension, oil dispersible powder, concentrated glue, pouring agent, seed coating agent, smear, film-forming oil agent, ultra-low volume liquid agent, steam release agent;The insecticide composition is applicable to plant pests selected from the group consisting of fall armyworm, red spider, East Asian migratory locust, cloud-spotted locust, Chinese rice locust, Japanese yellow-spine locust, single-spined mole cricket, oriental mole cricket, rice thrips, tobacco thrips, greenhouse thrips, rice tube thrips, wheat tube thrips, greenhouse whitefly, Bemisia tabaci, black-tailed leafhopper, green leafhopper, cotton leafhopper, spotted wax cicada, brown planthopper, white-backed Planthoppers, gray planthoppers, sugarcane flat-horned planthoppers, cotton aphids, wheat aphids, wheat long-tubed aphids, peach aphids, sorghum aphids, radish aphids, cotton scale, mulberry shield scale, arrow-pointed shield scale, pear round scale, white wax insect, red wax scale, Korean ball-hard scale, pear web bug, banana web bug, fine-horned flower bug, tiny flower bug, needle-edge bug, rice spider bug, rice brown bug, rice black bug, rice green bug, green blind bug, alfalfa blind bug, Middle black blind bug, large lacewings, beautiful lacewings, Chinese lacewings, grain moth, clothes moth, yellow thorn moth, brown thorn moth, flat thorn moth, wheat moth, cotton bollworm, sweet potato moth, diamondback moth, peach borer, soybean borer, peach borer, apple top leaf roller, brown-banded long leaf roller, quasi-small yellow leaf roller, striped stem borer, bean pod borer, corn borer, yellow stem borer, cabbage borer, rice leaf roller , striped borer, cotton leaf roller, peach borer, armyworm, armyworm, rice borer, cotton bridge worm, beet armyworm, greater stem borer, cotton bollworm, Dingdian diamond drill, small cutworm, large cutworm, yellow cutworm, thief moth, gypsy moth, sweet potato hawkmoth, bean hawkmoth, straight-striped rice hesperid, hidden grain hesperid, citrus swallowtail, jade-belt butterfly, cabbage butterfly, ramie red admiral, ramie yellow admiral Butterfly, bean lycopersicum, Venus carabiner, wrinkled carabiner, wheat ear carabiner, groove wireworm, fine-breasted wireworm, grain spot beetle, black skin beetle, citrus small jellyfish, golden edge jellyfish, yellow mealworm, black mealworm, red flour beetle, mixed flour beetle, copper green beetle, dark beetle, North China black gill beetle, mulberry longhorn beetle, star longhorn beetle, orange brown longhorn beetle, pink neck longhorn beetle, big monkey leaf beetle, small Ape leaf beetle, yellow melon beetle, yellow striped flea beetle, mung bean weevil, pea weevil, broad bean weevil, corn weevil, rice weevil, wheat sawfly, pear fruit bee, yellow-banded ichneumon wasp, white-star ichneumon wasp, hanging cocoon ichneumon wasp, cotton bollworm tooth-lipped ichneumon wasp, black-spotted warty ichneumon wasp, mosquito, fly, horsefly, red wheat midge, yellow wheat midge, rice gall midge, citrus fruit fly, melon fruit fly, wheat leaf ash leafminer, American spotted leafminer flies, bean stalk black miners, wheat stalk flies, seed flies, onion flies, radish flies, umbrella skirt chasing flies, corn borer flies, armyworms; the insecticide composition is applicable to plants selected from: rice, wheat, barley, oats, corn, sorghum, sweet potatoes, potatoes, cassava, soybeans, snow peas, broad beans, peas, mung beans, adzuki beans, cotton, sericulture, peanuts, rapeseed, sesame, sunflower, beet, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rapeseed, onion, garlic, watermelon, melon, cantaloupe, papaya, apple, citrus and peach trees, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, bonsai. ;

[0085] Example 8: Application of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in combination with a fungicide in the prevention and treatment of agricultural, forestry and horticultural plant diseases:

[0086] The amide derivative I containing 3,4-dichloroisothiazole of the present invention is combined with any one or two of commercial fungicides to form a fungicide composition for preventing and controlling agricultural, forestry and horticultural plant diseases. The commercial fungicide is selected from: benzothiadiazole, thiazolamide, thiazolamide, isothiazolamide, viravir, anthofin, ningnanmycin or salicylic acid, cymoxanil, thiram, zinc thiram, mancozeb, fosetyl-aluminum, methyl thiophanate, chlorothalonil, dichlorvos, procymidone, fenpropidin, methyl thiophanate, thiophanate, metalaxyl-M, flumorph, dimethomorph, high-efficiency metalaxyl, high-efficiency bensulfuron, dichlorocyanamide, sulfaquinoxaline, sulfaquinoxaline, thiofluanid, chlorothalonil, cyclamic acid, cyanamide, silthiophanate, carboxin, oxycarboxin, wheat Rust-ling, furamide, oxadiazine, flutolanil, furopyram, thiofuran, boscalid, penthiopyrad, pyraclostrobin, bixafen, fluopyram, fluoxazolidinone, fluopyram, fluopyram, fluopyram anilide, phenyltrichloroethane, isopropylthiopyrad, fluopyram hydroxylamide, fluphenyletheramide, fluopyram, dimethomorph, oxadiazine, ethylpyraclostrobin, isopropylthiopyrad, fluopyram, fluopyram, oxadiazine, ethylpyraclostrobin, isopropylthiopyrad, fluopyram, fluopyram, fluopyram, pyraclostrobin, pyraclostrobin Ester, ethersstrobin, fluoxastrobin, ethersstrobin, benzyloxystrobin, oxazolidinone, pyraclostrobin, oxazolidinone, oxazolidinone, oxazolidinone, oxazolidinone, oxazolidinone, oxazolidinone, oxazolidinone, cyproconazole, difenoconazole, diniconazole, high-efficiency diniconazole, fluoxiconazole, nitrobenazole, fluquinconazole, flusilazole, flutriafol, hexaconazole, imipenem, phyconazole, metconazole, myclobutanil, penconazole, propiconazole , prothioconazole, silifonazole, tebuconazole, tetrafluthrin, triadimenol, chloranil, bifenthrin, thiabendazole, wheat spike, imazalil, high-efficiency imazalil, prochloraz, trifloxystrobin, cyazofamid, imidacloprid, oxamidazole, rice blast ester, oxadiazine, pyraclostrobin, oxadiazine, oxadixyl, trifloxystrobin, thiabendazole ... Morpholine, fenchlorpyrifos, fludioxonil, fluazinam, pyraclostrobin, cyclamoxadone, fluopicolide, pyraclostrobin, cyprodinil, fluopicolide, thiophanate-methyl, pyraclostrobin, chlorfenapyr, flufenapyr, mite-killing agent, dicyanoanthraquinone, ethoxyquinoline, hydroxyquinoline, propoxyquinoline, phenoxyquinoline, ethotripsy, isopropanil, benzathiapiprolin, cyproconazole, sulfamethoxam, dithiocarb, isoflurane, isoflurane, chloranil ... Rice blast net, pyraclofos, methyl tolclofos, blasticide, kasugamycin, polyoxin, polyoxin, validamycin, Jinggangmycin, streptomycin, metalaxyl, furalaxyl, bensulfuron, furamide, carbendazim, benomyl, methyl thiophanate, triadimefon, pyrimidine sulfonate, dimethylpyrimidine, pyrimidine, captan, captan, folpet, vinyl sclerotin, fluchloric acid sclerotin, sclerotin, thiophanate-methyl, rice blast, rice blast net, leaf blight, pentachloronitrobenzene, propineb, fosetyl-aluminum, sulfur, Bordeaux mixture, copper sulfate, copper oxychloride, cuprous oxide, copper hydroxide, mefenamic acid, pencuron, pyridamyl, tetrachlorophthalide, pyroquinone, spiroxanil, tricyclazole, quinacridone, polypyrrolidone, biguanide salt, biguanide octylamine, chlornitrile, benzylsulfuron, toluenesulfuron, indole esters,Sodium sulfamethoxam, quinclorac, allylbenzazole, bronopol, iodomethane, metamethylenetetracycline, dazomethane, dichloroisopropyl ether, thiathion, fenthiophos, cypermethrin, chloranil, butylthiophos, oxamyl, sulfuryl fluoride, dichloropropylene, dichloroisonicotinic acid, allylisothiazole; the total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the fungicide composition is 1%-90%, and the amount percentage of the amide derivative I containing 3,4-dichloroisothiazole in the fungicide composition is 1%-90%. 1%:99% to 99%:1%; the dosage form of the fungicide composition is selected from: seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granules, fine granules, soluble concentrate, poison valley, block poison bait, granular poison bait, sheet poison bait, concentrated poison bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot fog, cold fog, aerosol, solid / liquid mixed preparation, liquid / liquid mixed preparation, Solid / solid mixed preparations, lacquers, microgranules, tracking powders, oil suspensions, oil-dispersible powders, concentrated gels, pouring agents, seed coatings, smears, film-forming oils, ultra-low volume liquids, and steam release agents; the plant diseases applicable to the fungicide composition are selected from: rice seedling rot, tomato root rot, potato late blight, tobacco black shank, millet powdery mildew, grape downy mildew, lettuce downy mildew, cucumber downy mildew, and cucumber anthracnose; the plants applicable to the fungicide composition are selected from: rice, wheat, barley, oats, corn, Sorghum, sweet potato, potato, cassava, soybean, snow pea, broad bean, pea, mung bean, adzuki bean, cotton, sericulture, peanut, rapeseed, sesame, sunflower, beet, sugar cane, coffee, cocoa, ginseng, Fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rapeseed, onion, garlic, watermelon, melon, cantaloupe, papaya, apple, citrus and peach, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, bonsai.

[0087] Example 9: Application of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in combination with an anti-plant virus agent in the prevention and treatment of viral diseases of agricultural, forestry and horticultural plants:

[0088] The amide derivative I containing 3,4-dichloroisothiazole of the present invention is combined with any one or two of commercial antiviral agents to form an antiviral composition for preventing and controlling viral diseases of agricultural, forestry and horticultural plants. The commercial antiviral agent is selected from: benzothiadiazole, thiazolamide, isothiazolamide, viravirin, anthofin, ningnanmycin, methiazolamide or salicylic acid, pyrimidine, dichloroisonicotinic acid, allylisothiazole, jinggangmycin, and guanidine hydrochloride; the total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in the antiviral composition is 1%-9% 0%, the ratio of the amide derivative I containing 3,4-dichloroisothiazole of the present invention to the aforementioned commercial anti-plant virus agent is 1%:99% to 99%:1% by mass; the dosage form processed by the anti-virus composition is selected from: seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granules, fine granules, soluble concentrate, poison valley, block bait, granular bait, sheet bait, concentrated bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot fog, cold fog agent, aerosol, solid / liquid mixed agent, liquid / liquid mixed agent, solid / solid mixed agent, lacquer, microgranules, tracking powder, oil suspension, oil dispersible powder, concentrated glue, pouring agent, seed coating agent, smear, film-forming oil agent, ultra-low volume liquid agent, steam release agent; the virus diseases controlled by the antiviral composition are selected from: rice dwarf disease, yellow dwarf disease, stripe leaf blight, tomato fern leaf virus disease, pepper mosaic virus disease, tobacco vein necrosis virus disease, corn dwarf mosaic disease, cauliflower mosaic virus, citrus virus disease, Jianlan orchid leaf virus, Jianlan ringspot virus; the antiviral composition is used The plants for prevention and control are selected from: rice, wheat, barley, oats, corn, sorghum, sweet potato, potato, cassava, soybean, snow pea, broad bean, pea, mung bean, adzuki bean, cotton, sericulture, peanut, rapeseed, sesame, sunflower, beet, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomato, pepper, radish, cucumber, cabbage, celery, mustard tuber, beet, rapeseed, onion, garlic, watermelon, melon, cantaloupe, papaya, apple, citrus and peach, tea, wild vegetables, bamboo shoots, hops, pepper, banana, papaya, orchid, bonsai.

[0089] Example 10: Application of the amide derivative I containing 3,4-dichloroisothiazole of the present invention in combination with acaricides in preventing and controlling mite damage in agriculture, forestry and horticultural plants:

[0090] The amide derivative I containing 3,4-dichloroisothiazole of the present invention is combined with any one or two of commercial acaricides to form a miticide composition for preventing and controlling mite pests in agriculture, forestry and horticultural plants. The commercial acaricide is selected from the group consisting of dichlorvos, heptylphos, cypermethrin, dibromophos, pyrifos, chlormethoxam, ethion, cypermethrin, phosalone, methyl pyrifos, quinalphos, aphidox, chlormethoxam, chlormethoxam, phosmet, flumethoxam, acralthrin, bifenthrin, cyhalothrin, cyhalothrin, cyhalothrin, cyhalothrin, cyhalothrin, cyhalothrin, bifenthrin, fenthiocarb, butanone, oxamyl, cypermethrin, long-acting cypermethrin, benomyl, chlormethoxam, cypermethrin, benzyl benzoate, bromothrin Ester, butyric acid ester, acequinoxaline, fluazifop, flufenoxuron, liuyangmycin, cypermethrin, thuringin, acaricide, liuyangmycin, avermectin, doramectin, eprinomectin, ivermectin, selamectin, moxidectin, pyrethrin, nicotine, matrine, azadirachtin, rotenone, tebufenamide, pyridabenzan, cypermethrin, cypermethrin, cypermethrin, cypermethrin, cypermethrin, hexythiazolin, spirocyclopent, pyrimidifen, cypermethrin, cypermethrin, propargite, pyridabenzan; the total mass percentage of the amide derivative I containing 3,4-dichloroisothiazole in the acaricide composition is 1%-90%, and the ratio of the amide derivative I containing 3,4-dichloroisothiazole to the commercial acaricide is 1%:99% to 99%:1% by mass; the acaricide composition The dosage form of the processed material is selected from: seed treatment emulsion, aqueous emulsion, microemulsion, suspoemulsion, capsule suspension, water-soluble granule, fine granule, soluble concentrate, poisonous grain, block poison bait, granular poison bait, sheet poison bait, concentrated poison bait, slow-release block, electrostatic spray, oil-in-water emulsion, smoke can, smoke candle, smoke tube, smoke stick, smoke sheet, smoke pill, gasifier, ointment, hot mist, cold mist, aerosol, solid / liquid mixed agent, liquid / liquid mixed agent, solid / solid mixed agent, lacquer, microgranule, tracking powder, oil suspension, oil dispersible powder, concentrated glue, pouring agent, seed coating agent, smear, film-forming oil, ultra-low volume liquid, steam release agent; the mite pests controlled by the acaricide composition are selected from: the mite pests are selected from Tetranychus, Tenebriophyidae, Furonematodes , Tetranychus genus, and Tetranychus genus, which are pests of the family Acaridae, Tetranychus genus, and the family Acaridae. These pests are global agricultural pests, forestry pests, gardening pests, and sanitary pests. The plants for which the acaricidal composition is used to control are selected from the group consisting of rice, wheat, barley, oats, corn, sorghum, sweet potatoes, potatoes, cassava, soybeans, snow peas, broad beans, peas, mung beans, adzuki beans, cotton, sericulture, peanuts, rapeseed, sesame, sunflowers, beets, sugarcane, coffee, cocoa, ginseng, fritillaria, rubber, coconut, oil palm, sisal, tobacco, tomatoes, peppers, radishes, cucumbers, cabbages, celery, mustard tubers, beets, rapeseed, onions, garlic, watermelons, melons, cantaloupes, papayas, apples, citrus and peach trees, tea, wild vegetables, bamboo shoots, hops, peppers, bananas, papayas, orchids, and bonsai.

[0091] Industrial Applicability

[0092] The present invention provides an amide derivative containing 3,4-dichloroisothiazole; the derivative of the present invention can regulate the biological activities of agricultural, horticultural, sanitary and forestry plant pests and plant pathogens, can be used in the agricultural, horticultural and forestry fields to kill insects, mites, sterilize, resist plant viruses, and induce plants to produce disease resistance, and has good economic value and application prospects.

[0097] Table 3 Antibacterial activity of the amide derivatives I containing 3,4-dichloroisothiazole of the present invention (inhibition rate at 50 μg / ml / %)

[0098] Serial number Compound No. As Bc Ca F Pp Rs Ss 1 I-1 30 42 29 10 19 26 28 2 I-2 51 56 43 42 49 51 37 3 I-3 34 44 23 8 26 0 21 4 I-4 29 15 26 13 9 0 2 5 I-5 52 46 28 39 41 50 36 6 I-6 49 68 28 24 39 45 31 7 I-7 42 20 29 4 13 0 6 8 I-8 28 35 24 4 17 10 16 9 I-9 38 53 30 18 28 34 31 10 I-10 38 31 34 18 28 10 26 11 I-11 43 66 43 26 44 47 47 12 I-12 37 28 28 19 28 8 22 13 I-13 29 19 23 0 17 0 10 14 I-14 24 21 32 10 17 22 23 15 MeJA 5 0 17 15 9 7 5 16 BTH 13 17 18 12 19 74 5 17 TDL 43 55 43 42 44 65 43 18 ISO 9 36 17 15 17 34 5

[0099] As: Tomato early blight pathogen, its Latin name is: Alternaria solani, Bc: Cucumber gray mold pathogen, its Latin name is: Botrytis cinerea, Ca: Peanut brown spot pathogen, its Latin name is: Cercospora arachidicola, Fg: Grainaceous fusarium pathogen, its Latin name is: Fusarium graminearum, Pp: Apple ring rot pathogen, its Latin name is: Physalosporapiricola, Rs: Rice sheath blight pathogen, its Latin name is: Rhizoctonia solani, Ss: Rapeseed sclerotinia pathogen, its Latin name is: Sclerotinia sclerotiorum.

[0100] Table 4 In vivo activity of the amide derivatives I containing 3,4-dichloroisothiazole of the present invention in inducing Arabidopsis thaliana against Arabidopsis thaliana (inhibition rate / %)

[0101] Serial number Compound No. Concentration (μmol / L) Inhibition rate 1 I-1 50 98 2 I-1 10 45 3 I-2 50 97 4 I-2 10 57 5 I-3 50 94 6 I-3 10 55 7 I-4 50 100 8 I-4 10 93 9 I-5 50 98 10 I-5 10 66 11 I-6 50 94 12 I-6 10 63 13 I-7 50 70 14 I-8 50 97 15 I-8 10 62 16 I-9 50 100 17 I-9 10 64 18 I-10 50 87 19 I-10 10 62 20 I-11 50 100 21 I-11 10 61 22 I-12 50 100 23 I-12 10 75 24 I-13 50 100 25 I-13 10 63 26 I-14 50 100 27 I-14 10 94 28 ISO 50 38 29 ISO 10 13 30 BTH 50 99 31 BTH 10 91 32 MeJA 50 26

Claims

1. A class of amide derivatives containing 3,4-dichloroisothiazole, characterized in that It contains 3,4-dichloroisothiazole and amide at the same time, and has the general structural formula shown in Formula I: I: Among them, R 1 , R 2 , R 3 Selected from: substituted alkyl, substituted alkenyl, hydrogen, substituted alkynyl, substituted cycloalkyl, substituted cycloalkenyl, substituted cycloalkynyl, substituted alkoxy, substituted alkenyloxy, substituted alkynyloxy, substituted phenyl, substituted heterocyclyl; The heterocyclic group is selected from: furanyl, thienyl, imidazolyl, pyrazolyl, pyridyl, pyranyl, indolyl, pyrimidinyl, triazine, isoindolyl and other nitrogen- or / and sulfur-containing three-membered ring group, four-membered ring group, five-membered ring group, six-membered ring group; R 3 Also selected from: Li, Na, K, n is selected from 1, 3, and 4; The above substituents are preferably: R 1 Selected from: 1-methylethyl, 1-methylpropyl, hydrogen, 2-(methylthio)ethyl, imidazole-4-methyl, 2-methylpropyl, indole-3-methyl, 3-methoxy-3-oxopropyl, methyl, benzyl, cyclohexylmethyl, methyl, benzyl, p-phenolmethyl, 2-amino-2-oxoethyl, hydroxymethyl, ethoxy, 3-guanidinopropyl, 4-aminobutyl, carboxymethyl; R 2 is selected from hydrogen, methyl; R 3 Selected from hydrogen, sodium, methyl, ethyl, propyl, butyl, isopropyl; n is selected from 1, 3, 4.

2. The specific synthetic route of the amide derivative I containing 3,4-dichloroisothiazole according to claim 1 is as follows: The substituent R 1 , R 2 , R 3 The definition of as in claim 1; The specific synthesis method of the amide derivative I containing 3,4-dichloroisothiazole according to claim 1 is as follows: The specific synthesis method is as follows: A. Preparation of Compound I: Compound I is prepared by reacting 3,4-dichloroisothiazole-5-carbonyl chloride and an amino acid or an ester of an amino acid or a salt of an amino acid: at room temperature, add 1 equivalent of carbamate hydrochloride 2 to dichloromethane, then add 2 equivalents of triethylamine, stir at room temperature for 1 minute, add 1.1 equivalents of compound 1, stir at room temperature for 6 hours, add 20 ml of sodium bicarbonate solution to quench, extract the aqueous phase with dichloromethane, combine the organic phases, wash the organic phases three times with saturated brine, and dry with anhydrous sodium sulfate, remove the solvent under reduced pressure, and purify the residue by 200-300 mesh silica gel column chromatography, the eluent is ethyl acetate / petroleum ether, to obtain an amide derivative I containing 3,4-dichloroisothiazole; the carbamate hydrochloride is selected from: 2-amino-3-phenylpropionic acid methyl ester hydrochloride, 1-aminocyclopropane-1-carboxylic acid ethyl ester hydrochloride, cycloleucine methyl ester hydrochloride, methyl 2-aminoisobutyrate hydrochloride, methyl 2-amino-3-cyclohexylpropionate hydrochloride, methyl 1-aminocyclohexanecarboxylate hydrochloride, methyl L-valine hydrochloride, methyl L-isoleucine hydrochloride, methyl L-methionine hydrochloride, methyl L-histidine dihydrochloride, tert-butyl L-leucine hydrochloride, methyl L-tryptophan hydrochloride, dimethyl L-glutamic acid hydrochloride, methyl glycine hydrochloride, methyl L-alanine hydrochloride, methyl L-phenylalanine hydrochloride, methyl L-tyrosine hydrochloride, methyl L-asparagine hydrochloride, methyl L-serine hydrochloride, methyl L-threonine hydrochloride, methyl L-arginine hydrochloride, methyl L-lysine hydrochloride, methyl L-aspartate hydrochloride, methyl L-proline hydrochloride, D-3-aminobutyric acid, β-aminobutyric acid.

3. Use of the amide derivative I containing 3,4-dichloroisothiazole according to claim 1 in the preparation of an agricultural fungicide, wherein the fungicide controls and prevents the following objects: tomato early blight, cucumber gray mold, peanut brown spot, graminearum Fusarium, apple ring rot, rice sheath blight, rapeseed sclerotinia, and plant viral diseases.

4. Use of the amide derivative I containing 3,4-dichloroisothiazole according to claim 1 in the preparation of a plant activator, wherein the plant activator prevents and treats the following diseases: tomato early blight, cucumber gray mold, peanut brown spot, graminearum Fusarium wilt, apple ring rot, rice sheath blight, rapeseed sclerotinia, and plant viral diseases.

5. An agricultural fungicidal composition, comprising the amide derivative containing 3,4-dichloroisothiazole as claimed in claim 1 as an active ingredient; the composition comprises 0.1% to 99.9% by weight of the active ingredient, 99.9% to 0.1% by weight of a solid or liquid adjuvant, and 0 to 25% by weight of a surfactant.

6. A plant activation composition comprising the amide derivative containing 3,4-dichloroisothiazole as claimed in claim 1 as an active ingredient; the composition comprises 0.1% to 99.9% by weight of the active ingredient, 99.9% to 0.1% by weight of a solid or liquid adjuvant, and 0 to 25% by weight of a surfactant.

7. An agricultural fungicide compound composition, comprising the amide derivative containing 3,4-dichloroisothiazole as claimed in claim 1 and other commercial fungicides as active ingredients; the mass percentage of the active ingredient containing the amide derivative of 3,4-dichloroisothiazole and the other commercial fungicides is 1%:99% to 99%:1%, and the compound composition contains 1% to 99% by weight of the active ingredient, 99% to 1% by weight of a solid or liquid adjuvant, and 0 to 25% by weight of a surfactant.

8. An agricultural insecticide and acaricide compound composition, comprising the amide derivative containing 3,4-dichloroisothiazole according to claim 1 and other commercial insecticides and acaricides as active ingredients; the mass percentage of the active ingredient containing the amide derivative of 3,4-dichloroisothiazole and the other commercial insecticides and acaricides is 1%:99% to 99%:1%, and the compound composition comprises 1% to 99% by weight of the active ingredient, 99% to 1% by weight of a solid or liquid adjuvant, and 0 to 25% by weight of a surfactant selected from the group consisting of.

9. A composite composition of anti-plant virus agents, comprising the amide derivative containing 3,4-dichloroisothiazole according to claim 1 and other commercial anti-plant virus agents as active ingredients; the mass percentage of the active ingredient containing the amide derivative of 3,4-dichloroisothiazole and the other commercial anti-plant virus agents is 1%:99% to 99%:1%, and the composite composition contains 1% to 99% by weight of the active ingredient, 99% to 1% by weight of a solid or liquid adjuvant, and 0 to 25% by weight of a surfactant selected from.

10. A plant activator compound composition, comprising the amide derivative containing 3,4-dichloroisothiazole according to claim 1 and other commercial plant activators as active ingredients; the mass percentage of the active ingredient containing the amide derivative of 3,4-dichloroisothiazole and the other commercial plant activators is 1%:99% to 99%:1%, and the compound composition comprises 1% to 99% by weight of the active ingredient, 99% to 1% by weight of a solid or liquid adjuvant, and 0 to 25% by weight of a surfactant selected from the group consisting of.

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