CN103193769A

CN103193769A - 4-methyl-1,2,3-thiadiazole-5-triazole compound as well as preparation method and use thereof

Info

Publication number: CN103193769A
Application number: CN2013101273321A
Authority: CN
Inventors: 范志金; 李岳东; 陈旭艳; 王盾; 房震; 姬晓恬; 华学文; 毛武涛; 宗广宁; 李凤云
Original assignee: Nankai University
Current assignee: Nankai University
Priority date: 2013-04-15
Filing date: 2013-04-15
Publication date: 2013-07-10

Abstract

The invention provides a 4-methyl-1,2,3-thiadiazole-5-triazole compound as well as a preparation method and use thereof, and relates to a heterocyclic compound containing 1,2,3-thiadiazole. The heterocyclic compound has a chemical structural general formula shown in a formula I. The invention discloses a structural general formula of the compound, a synthetic method, and use as pesticide, acaricide and germicide, and a processing technology for preparing the pesticide, the acaricide and the germicide by mixing with an agriculturally acceptable auxiliary agent or a synergist, and also discloses use of these compounds combined with the commodities such as the pesticide, the acaricide, the germicide, acetylglucosyl bromide and a plant activator in prevention and treatment of diseases, insect pests, mite damages and virus diseases in agriculture, forestry and gardening, and the preparation method.

Description

One class 4-methyl isophthalic acid, 2,3-thiadiazoles-5-triazole class compounds and its production and use

Technical field

Technical scheme of the present invention relates to 1,2,4-triazole compounds, is specially the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-triazole compounds.

Background technology

1,2,4-triazole class compounds since the biological activity of its wide spectrum with and wide application prospect, quite be subjected to people's favor always.That 1,2,4-triazole class compounds mainly demonstrates is antimycotic, plant-growth regulator and weeding activity, but some triazole class compounds has concurrently or has an insecticidal activity (Du sea hall .1, synthetic and the biological activity [D] of 2,4-triazole derivative. University Of Tianjin, 2009).For example, be used for the control of garden crop Powdery Mildew in the spirit of prestige bacterium, have desinsection, acaricidal activity concurrently; Triazophos be exploitation in 1970 a kind of broad spectrum insecticide, kill mite and nematocides, still using so far; Isazofos is the kind of vapour Ba in 1973-Jia Ji company exploitation, it have tag, stomach toxicity and systemic action, be used for corn, cotton, paddy rice, beet and vegetables, prevent and treat multiple insect pest; The compd A of Rohm Hass company exploitation in 1988 is a kind of selectivity systemic insecticide; it has rapid inhibitory effect to the insect Pseudocholinesterase, can be used for preventing and treating black peach aphid, cotten aphid etc., and soil pesticide can be prevented and treated the leaf-feeding aphid; medicament is migration up and down in plant, and whole strain crop is had provide protection.

Triaxamate (Triazamate), chemical name: 3-tertiary butyl-1-N, N-dimethylamino formyl-1H-1,2,4-triazole-5-ethyl thioglycolate is that the triazole species promoted of Dow company is efficient, highly selective, tags and the obligate aphicide (EP0213718) of characteristics such as interior suction, aphid preventive effect to various crop is good, two-way conduction in plant materials, but soil application, but also foliage spray.To Mammals and people and animals' low toxicity, safety, better to cotton, wheat aphid preventive effect.

The research of relevant thiadiazoles mainly concentrates on 1,3,4-thiadiazoles derivative, 1,2,5-thiadiazoles derivative and 1,2, on the 4-thiadiazoles derivative, although the research of 1,2,3-thiadiazoles derivative activity report is less relatively, but 1,2,3-thiadiazole compound has biological activity (Bakulev, et al.Newyork:John Wiley﹠amp widely; Sons, Inc, 2004), at present, 1,2,3-thiadiazoles derivative commercial kind in medicine and agricultural chemicals is few, agriculture field application have only cotton defoliant--disleave spirit (N-phenyl-N '-1,2,3-thiadiazoles-5-urea, TDZ), plant activator--Acibenzolar (phendioxin, 2,3-thiadiazoles-7-thiocarboxylic acid methyl esters, BTH), rice field sterilant--tiadinil (3 '-chloro-4,4 '-dimethyl-1,2,3-thiadiazoles-5-formylaniline, TDL).Contriver's research and design in earlier stage is synthetic and found that the first thiophene lures the inducing anti-disease activity of amine, at present just in the industrialization development process.

In order to seek 1,2 of high biological activity more, 3-thiadiazole new compound, the present invention is with 1,2,3-thiadiazoles ring introduces 1,2, in the 4-triazole molecule, a class 4-methyl isophthalic acid, 2,3-thiadiazoles-5-triazole class compounds have been synthesized in design, and carried out the bioactive screening of system, in the hope of providing the candidate compound for novel pesticide initiative research.

Summary of the invention

Technical problem to be solved by this invention is: new 4-methyl isophthalic acid is provided, 2,3-thiadiazoles-5-triazole class compounds synthetic method, provide this compounds to suppress biological activity and the measuring method of agricultural and gardening and forestry plant pathogen, insect and evil mite, the middle application of these compounds in agriculture field and gardening field and field of forestry is provided simultaneously.

The present invention solves this technical problem the technical scheme that adopts: the 4-methyl isophthalic acid with agriculture field, gardening field, field of forestry desinsection, acaricidal activity, fungicidal activity, anti-phytoviral activity, inducing plant generation anti-disease activity, the chemical structure of general formula of 2,3-thiadiazoles-5-triazole class compounds is seen formula I:

Wherein, RCO is selected from: N, the N-formyl-dimethylamino, hydrogen, tertiary butyl formyl radical, the cyclopentyl ethanoyl, cyclopropane carbonyl, the cyclobutylmethyl acyl group, the cyclohexyl formyl radical, the 2-furancarbonyl, the 2-Thenoyl, 2-chloropyridine-3-formyl radical, 6-chloropyridine-3-formyl radical, to the tert.-butylbenzene formyl radical, the 2-nitro benzoyl, the 3-nitro benzoyl, 3, the 5-dinitrobenzoyl, the 2-fluoro benzoyl, the 3-fluoro benzoyl, the 2-chlorobenzene formacyl, the 3-chlorobenzene formacyl, the 4-chlorobenzene formacyl, the 2-methyl benzoyl, the 3-methyl benzoyl, the 4-methyl benzoyl, 3,5-dimethylbenzoyl, 2-trifluoromethyl benzoyl, 3-trifluoromethyl benzoyl, 4-trifluoromethyl benzoyl, the 2-anisoyl, the 3-anisoyl, the 4-anisoyl, 4-cyano group benzoyl, ethoxycarbonylmethyl group; N=0,1,2.

Chemical structure of general formula is seen the 4-methyl isophthalic acid of formula I, and 2,3-thiadiazoles-5-triazole class compounds specifically is divided into V, VI, VII, VIII, IX, X6 kind form:

4-methyl isophthalic acid of the present invention, the synthetic method of 2,3-thiadiazoles-5-triazole class compounds I is as follows:

Wherein, RCO is selected from: N, the N-formyl-dimethylamino, hydrogen, tertiary butyl formyl radical, the cyclopentyl ethanoyl, cyclopropane carbonyl, the cyclobutylmethyl acyl group, the cyclohexyl formyl radical, the 2-furancarbonyl, the 2-Thenoyl, 2-chloropyridine-3-formyl radical, 6-chloropyridine-3-formyl radical, to the tert.-butylbenzene formyl radical, the 2-nitro benzoyl, the 3-nitro benzoyl, 3, the 5-dinitrobenzoyl, the 2-fluoro benzoyl, the 3-fluoro benzoyl, the 2-chlorobenzene formacyl, the 3-chlorobenzene formacyl, the 4-chlorobenzene formacyl, the 2-methyl benzoyl, the 3-methyl benzoyl, the 4-methyl benzoyl, 3,5-dimethylbenzoyl, 2-trifluoromethyl benzoyl, 3-trifluoromethyl benzoyl, 4-trifluoromethyl benzoyl, the 2-anisoyl, the 3-anisoyl, the 4-anisoyl, 4-cyano group benzoyl, ethoxycarbonylmethyl group; N=0,1,2;

Specifically be divided into following steps:

A.4-methyl isophthalic acid, the preparation of 2,3-thiadiazoles-5 formyl hydrazine II:

With the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-ethyl formate 17 grams, i.e. 0.1 mole and 80% hydrazine hydrate, 9.3 grams, namely 0.15 mole, add in 100 milliliters the flask, add 50 milliliters of n-propyl alcohols in flask, stir it is mixed, oil bath reflux 4 hours, then with its cooling, the concentrating under reduced pressure desolventizing, have yellow solid to separate out, suction filtration also gets compound 4-methyl isophthalic acid, 2 with the washed with isopropyl alcohol solid, 3-thiadiazoles-5 formyl hydrazine II, oven dry is 10.6 grams, productive rate is 82.5%; The amount of intermediate II preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle;

B.4-methyl isophthalic acid, the preparation of 2,3-thiadiazoles-5-formamido group thiocarbamide III

Compound I I15.8 is restrained, i.e. 0.1 mole and potassium sulfocyanate 19.4 grams, namely 0.2 mole, add in 25 milliliters the flask, add 10 milliliters of hydrochloric acid solns: hydrochloric acid soln is made up of 2 milliliter of 37% concentrated hydrochloric acid and 8 ml waters, stirs it is mixed, reacted 4-5 hour down in 80-90 degree centigrade, the adularescent solid is separated out in the reaction process, and after the ice bath cooling, suction filtration gets solid chemical compound III, obtain 11.9 grams after the oven dry, productive rate is 55%; The amount of intermediate III preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle; Chemical structure and the physical and chemical parameter of intermediate III see Table 1;

C.3-sulfydryl-5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl)-2H-1, the preparation of 2,4-triazole IV

With compound III 2.17 grams, i.e. 10 mmoles, add in 100 milliliters the flask with the 5%NaOH40 milliliter, stirring mixes it, and back flow reaction 4-5 hour, then with its ice bath cooling, the hydrochloric acid soln that adds 2 mol is regulated pH=5, have flaxen solid to separate out, suction filtration also uses the saturated common salt water washing to get compound IV 1.8 grams after the drying again, and productive rate is 85%; The amount of intermediate compound IV preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle; Chemical structure and the physical and chemical parameter of intermediate compound IV see Table 1;

D.5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl)-2H-1, the preparation of 2,4-triazole-3-ethyl thioglycolate V

With compound IV 0.39 gram, i.e. 2.0 mmoles, with salt of wormwood 0.41 gram, i.e. 3.0 mmoles, add in 25 milliliters the flask, add ethyl chloroacetate 0.24 gram simultaneously, namely 2.0 mmoles add 6.5 milliliters of dehydrated alcohols, stirring mixes it, oil bath back flow reaction 2 hours is removed ethanol with its decompression then, and the hydrochloric acid soln that adds 2 mol is regulated pH=5, again it is got organic layer with dichloromethane extraction, organic layer is used saturated sodium bicarbonate solution in succession, each washing of saturated nacl aqueous solution is once used anhydrous sodium sulfate drying then, and suction filtration is removed anhydrous sodium sulphate, filtrate decompression concentrates desolventizing, get compound V0.38 gram through 200～300 order purification by silica gel column chromatography, eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, productive rate are 67%; The amount of compound V preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle; Chemical structure and the physical and chemical parameter of compound V see Table 1;

E.5-(4-methyl isophthalic acid, 2,3-thiadiazoles)-2H-1, the preparation of 2,4-triazole-3-(Asia) sulfuryl ethyl acetate (VI) VII

At ice bath with under stirring, with compound V0.49 gram, namely 1.75 mmoles with 10 milliliters of methylene dichloride dissolvings, add MCPBA then in batches; When n=1, the MCPBA consumption is 1.75 mmoles; When n=2, the MCPBA consumption is 4.38 mmoles; Reaction mixture reaction 3 hours, the adularescent solid occurs in the reaction process; Concentrating under reduced pressure reaction solution behind the stopped reaction gets compound VI or VII through 200～300 order purification by silica gel column chromatography, and eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, and its productive rate is respectively 52.1% and 44.2%; The amount of compound VI or VII preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle; Chemical structure and the physical and chemical parameter of compound VI or VII see Table 1;

F.2-replacement-(5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl))-2H-1, the preparation of 2,4-triazole-3-ethyl thioglycolate VIII

Get in the flask that compound V2.0 mmole and triethylamine 4.0 mmoles join 25 milliliters, add the DMAP0.2 mmole, add 10 milliliters of 10 milliliters of anhydrous methylene chlorides or tetrahydrofuran (THF)s, stirring mixes it, drip 5 milliliters of the dichloromethane solution contain the RCOCl1.5 mmole or tetrahydrofuran (THF)s with addition funnel under the ice bath, dropwise under the normal temperature of back and reacted 4-5 hour, then reaction solution is diluted with 30 milliliters of methylene dichloride, use 2 mol HCl respectively, saturated sodium bicarbonate solution, each washing of saturated nacl aqueous solution once, use the anhydrous sodium sulfate drying organic layer then, concentrate, with 200-300 order silica gel column chromatography separating purification product VII I, eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, with the pure product calculated yield of gained; Its physical and chemical parameter and structural parameter see Table 1; The amount of compound VIII preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle;

G.5-(4-methyl isophthalic acid, 2,3-thiadiazoles)-2H-1, the preparation of 2,4-triazole-3-(Asia) sulfuryl ethyl acetate (IX) X

At ice bath with under stirring, with compound VIII 1.75 mmoles, with 10 milliliters of methylene dichloride dissolvings, add MCPBA then in batches; When n=1, the MCPBA consumption is 1.75 mmoles; When n=2, the MCPBA consumption is 4.38 mmoles; Reaction mixture reaction 3 hours, the adularescent solid occurs in the reaction process; Concentrating under reduced pressure reaction solution behind the stopped reaction gets compound I X or X through 200～300 order purification by silica gel column chromatography, and eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, calculate productive rate with its pure product of gained; The amount of compound I X or X preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle; Chemical structure and the physical and chemical parameter of compound I X or X see Table 1;

H.4-methyl isophthalic acid, the mensuration of 2,3-thiadiazoles-pathogenic fungi growth activity of 5-triazole class compounds I:

4-methyl isophthalic acid of the present invention, 2,3-thiadiazoles-5-triazole class compounds I sterilization or bacteriostatic activity adopt thalli growth rate assay method, detailed process is: get 5 milligrams of sample dissolution in an amount of dimethyl formamide, then with containing the medicament that a certain amount of polysorbas20 emulsifier aqueous solution is diluted to 500 mcg/ml, reagent agent is respectively drawn under aseptic condition in 1 milliliter of injection culture dish, add 9 milliliters of substratum more respectively, make 50 mcg/ml pastille flat boards after shaking up, do blank with the flat board that adds 1 milliliter of aqua sterilisa, punch tool with 4 millimeters of diameters cuts the bacterium dish along the mycelia outer rim, move on the pastille flat board, being equilateral triangle puts, every processing repeats 3 times, culture dish is placed on cultivation in 24 ± 1 degrees centigrade of constant incubators, colony diameter to be contrasted expands to 2-3 centimetre of " Invest, Then Investigate " and respectively handles bacterium dish expansion diameter, average, relatively calculate relative bacteriostasis rate with blank, for trying the kind that bacterial classification comprises most of phytopathogen of the actual generation in multiple representative field in China's agriculture production, its title and code name comprise AS: tomato early blight bacterium (Alternaria solani); BC: botrytis cinerea pers (Botrytis cinerea); CA: peanut Cercospora bacteria (Cercospora arachidicola); GZ: fusarium graminearum (Gibberella zeae); PI: phytophthora infestans (Phytophthora infestans (Mont.) de Bary); PP: ring rot of apple bacterium (Physalospora piricola); PS: Rhizoctonia solani Kuhn (Pellicularia sasakii); RC: cereal rhizoctonia (Rhizoctonia cerealis); SS: Sclerotinia sclerotiorum (Sclerotinia sclerotiorum).

I. the 4-methyl isophthalic acid that contains of the present invention, the mensuration of 2,3-thiadiazoles-aphid insecticidal activity of 5-triazole class compounds I:

4-methyl isophthalic acid of the present invention, the insecticidal activity screening method of 2,3-thiadiazoles-aphid larva of 5-triazole class compounds I is as follows: adopt pickling process, black bean aphid (Aphis laburni Kaltenbach) (ALK), the normal population of indoor feeding; Take by weighing 2.5 milligrams of test compounds in beaker, drip 1 N, dinethylformamide (DMF) adds 5 milliliters of acetone vibration dissolving samples, adds the solution to be measured that the water that tween 80 is arranged is mixed with 200 mcg/ml again; To have from basin, cutting for examination broad bean plant of at least 60 black bean aphids, in each soup to be measured, flooded for 5 seconds, take out and get rid of unnecessary soup gently, be inserted in and preserved moisture on the water saturated sponge, treat that the dried back of soup is with on the lens cover, the opening of lens upper end seals with gauze in case aphid escapes, and raises to place to check the aphid death state after 24 hours, and standard is: can creep with the examination worm and maybe can stand or six legs can strenuous exercises is worm alive; Be contrast with the clear water, the positive contrast of Provado, calculation correction mortality ratio.

J. 4-methyl isophthalic acid of the present invention, the mensuration of 2,3-thiadiazoles-5-triazole class compounds I antiviral activity:

4-methyl isophthalic acid of the present invention, the active screening method of 2,3-thiadiazoles-5-triazole class compounds I evoking tobacco resisting tobacco mosaic virus (TMV) is:

(1). standard plant activator: selecting tiadinil (TDL) (purity is greater than 99.5%) is the plant activator of standard;

(2) .4-methyl isophthalic acid, the screening method of 2,3-thiadiazoles-anti-TMV activity of 5-triazole class compounds I evoking tobacco: the mensuration of the direct antiviral activity that exsomatizes adopts half leaf method to carry out; It is common cigarette with the seedling age unanimity that live body is induced, 3 basins are one group, cigarette seedling respectively at inoculation pre-treatment in preceding 7 days, processing mode comprises: spray test compound solution 2 to 3 times, each 10 milliliters, or soil treatment, each 10 milliliters, measuring concentration is 50 mcg/ml, the 7th day frictional inoculation TMV on the tobacco leaf that newly grows, with the cigarette seedling place cultivate 3 days under its growth optimal temperature and illumination after, check incidence, comprehensive scab number is calculated as follows out test compound to the inducing anti-disease toxic effect fruit of TMV, and 3 repetition are established in each processing, blank to clear and standard medicament to clear water and the TDL of selecting respectively:

R = \frac{CK - I}{CK} \times 100

Wherein, R is that new compound is to the effect of inducing of the anti-TMV of tobacco, unit: %; CK is the average withered spot number of clear water contrast blade, unit: individual; I is for inducing the average withered spot number of handling rear blade, unit: individual through compound.

Except the mensuration of carrying out above-mentioned induced activity, carry out the 4-methyl isophthalic acid simultaneously, the mensuration of therapeutic activity, inactivate activity and the protection activity of 2,3-thiadiazoles-anti-TMV of 5-triazole class compounds I.

The invention has the beneficial effects as follows: the present invention is to the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-triazole class compounds I has carried out guide's optimization, and synthetic new compound carried out the screening of insecticidal activity and bacteriostatic activity and antiviral activity, carried out it simultaneously and mixed the research of using with common agricultural chemicals, this compounds can be used for control agriculture field and the plant pest in field of forestry and gardening field and the control of virus disease.

The present invention specifies the 4-methyl isophthalic acid more by specific preparation and biological activity determination embodiment, 2, synthetic and biological activity and the application thereof of 3-thiadiazoles-5-triazole class compounds I, described embodiment only is used for specifying the present invention and unrestricted the present invention, especially its biological activity only illustrates, and unrestricted this patent, embodiment is as follows:

Embodiment 1

The 4-methyl isophthalic acid, 2,3-thiadiazoles-5 formyl hydrazine II's is synthetic:

With the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-ethyl formate 17 grams, i.e. 0.1 mole and 80% hydrazine hydrate, 9.3 grams, namely 0.15 mole, add in 100 milliliters the flask, add 50 milliliters of n-propyl alcohols in flask, stir it is mixed, oil bath reflux 4 hours, then with its cooling, the concentrating under reduced pressure desolventizing, have yellow solid to separate out, suction filtration also gets compound 4-methyl isophthalic acid, 2 with the washed with isopropyl alcohol solid, 3-thiadiazoles-5 formyl hydrazine II, oven dry is 10.6 grams, productive rate is 82.5%;

Embodiment 2

Intermediate 4-methyl isophthalic acid, the synthetic and structure of 2,3-thiadiazoles-5-formamido group thiocarbamide III is identified

Compound I I15.8 is restrained, i.e. 0.1 mole and potassium sulfocyanate 19.4 grams, namely 0.2 mole, add in 25 ml flasks, add 10 milliliters of hydrochloric acid solns: this solution is formed stirring and evenly mixing by 2 milliliter of 37% concentrated hydrochloric acid and 8 ml waters, reacted 4-5 hour down in 80-90 degree centigrade, the adularescent solid is separated out in the reaction process, and after the ice bath cooling, suction filtration gets solid intermediate III, obtain 11.9 grams after the oven dry, productive rate is 55%; Chemical structure and the physical and chemical parameter of intermediate III see Table 1;

Embodiment 3

Intermediate 3-sulfydryl-5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl)-2H-1, the synthetic and structure of 2,4-triazole IV is identified

With intermediate III 2.17 grams, i.e. 10 mmoles, add in 100 milliliters the flask with the 5%NaOH40 milliliter, stir it is mixed, back flow reaction 4-5 hour, then with its ice bath cooling, the hydrochloric acid soln that adds 2 mol is regulated pH=5, has flaxen solid to separate out, and suction filtration is also used the saturated common salt water washing, get intermediate compound IV 1.8 grams again after the drying, productive rate is 85%; Chemical structure and the physical and chemical parameter of intermediate compound IV see Table 1;

Embodiment 4

5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl)-2H-1, the synthetic and structure of 2,4-triazole-3-ethyl thioglycolate V is identified

With compound IV 0.39 gram, i.e. 2.0 mmoles, with salt of wormwood 0.41 gram, i.e. 3.0 mmoles, add in 25 milliliters the flask, add ethyl chloroacetate 0.24 gram simultaneously, namely 2.0 mmoles add 6.5 milliliters of dehydrated alcohols, stirring mixes it, oil bath back flow reaction 2 hours is removed ethanol with its decompression then, and the hydrochloric acid soln that adds 2 mol is regulated pH=5, again it is got organic layer with dichloromethane extraction, organic layer is used saturated sodium bicarbonate solution in succession, each washing of saturated nacl aqueous solution is once used anhydrous sodium sulfate drying then, and suction filtration is removed anhydrous sodium sulphate, filtrate decompression concentrates desolventizing, get compound 5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl)-2H-1 through 200～300 order purification by silica gel column chromatography, 2,4-triazole-3-ethyl thioglycolate V0.38 gram, eluent is 3: 1 to 10: 1 60-90 of volume ratio degree centigrade sherwood oil: ethyl acetate, productive rate are 67%; Chemical structure and the physical and chemical parameter of compound V see Table 1;

Embodiment 5

5-(4-methyl isophthalic acid, 2,3-thiadiazoles)-2H-1, the synthetic and structure of 2,4-triazole-3-sulfoxide group ethyl acetate VI is identified:

At ice bath with under stirring, compound V0.49 is restrained, i.e. 1.75 mmoles, with 10 milliliters of methylene dichloride dissolvings, add MCPBA0.30 gram then, i.e. 1.75 mmoles, 3 hours reaction times in batches, the adularescent solid occurs in the reaction process, concentrating under reduced pressure reaction solution behind the stopped reaction concentrates the back with filtrate and gets compound VI with 200-300 order silica gel column chromatography separating purification, and eluent is that volume ratio is 3: 1 60-90 degree centigrade sherwood oil: ethyl acetate, altogether compound 5-(4-methyl isophthalic acid, 2,3-thiadiazoles)-and 2H-1,2,4-triazole-3-sulfoxide group ethyl acetate VI0.27 gram, productive rate is 52%; Its nuclear magnetic data (CDCl ₃, chemical shift): 1.282 (t, 3H, CH ₃, J=9.6Hz), 3.052 (s, 3H, CH ₃), 4.170-4.389 (m, 4H, CH ₂); Chemical structure and the physical and chemical parameter of compound VI see Table 1.

Embodiment 6

5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl)-2H-1, the synthetic and structure of 2,4-triazole-3-sulfoxide group ethyl acetate VII is identified

At ice bath with under stirring, compound V0.5 is restrained, i.e. 1.75 mmoles, with 10 milliliters of methylene dichloride dissolvings, add the MCPBA0.75 gram then in batches, namely 4.38 mmoles react after 3 hours concentrating under reduced pressure reaction solution behind the stopped reaction, filtrate is concentrated the back get compound 5-(4-methyl isophthalic acid with 200-300 order silica gel column chromatography separating purification, 2,3-thiadiazoles-5-yl)-and 2H-1,2,4-triazole-3-sulfoxide group ethyl acetate VII, eluent is that volume ratio is 3: 1 60-90 degree centigrade sherwood oil: ethyl acetate, get compound VI I0.24 gram, and productive rate is 44%; (nuclear magnetic data (DMSO-d6, chemical shift): 1.097 (t, 3H, CH ₃, J=9.4Hz), 2.973 (s, 3H, CH ₃), 4.055-4.126 (q, 2H, OCH ₂, J=10.0Hz), 4.896 (s, 2H, SCH ₂); Chemical structure and the physical and chemical parameter of compound VI I see Table 1.

Embodiment 7

2-replacement-(5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl))-2H-1, the synthetic and structure of 2,4-triazole-3-ethyl thioglycolate VIII is identified

Wherein, RCO is selected from: N, the N-formyl-dimethylamino, hydrogen, tertiary butyl formyl radical, the cyclopentyl ethanoyl, cyclopropane carbonyl, the cyclobutylmethyl acyl group, the cyclohexyl formyl radical, the 2-furancarbonyl, the 2-Thenoyl, 2-chloropyridine-3-formyl radical, 6-chloropyridine-3-formyl radical, to the tert.-butylbenzene formyl radical, the 2-nitro benzoyl, the 3-nitro benzoyl, 3, the 5-dinitrobenzoyl, the 2-fluoro benzoyl, the 3-fluoro benzoyl, the 2-chlorobenzene formacyl, the 3-chlorobenzene formacyl, the 4-chlorobenzene formacyl, the 2-methyl benzoyl, the 3-methyl benzoyl, the 4-methyl benzoyl, 3,5-dimethylbenzoyl, 2-trifluoromethyl benzoyl, 3-trifluoromethyl benzoyl, 4-trifluoromethyl benzoyl, the 2-anisoyl, the 3-anisoyl, the 4-anisoyl, 4-cyano group benzoyl, ethoxycarbonylmethyl group;

At 50 milliliters of three mouthfuls of round-bottomed flasks, get in the flask of 25 milliliters of compound V2.0 mmole and triethylamine 4.0 mmoles addings, add 0.2 mmole DMAP, 10 milliliters of anhydrous methylene chlorides, stirring and evenly mixing; Under the ice bath, drip 5 milliliters of dichloromethane solutions containing the RCOX1.5 mmole with addition funnel, dropwised under the normal temperature of back reaction 4-5 hour; Then reaction solution is diluted with 30 milliliters of methylene dichloride, respectively wash once with 2 mol HCl, saturated sodium bicarbonate solution, saturated nacl aqueous solution respectively, use the anhydrous sodium sulfate drying organic layer then, after concentrating, get compound 2-replacement-(5-(4-methyl isophthalic acid with 200-300 order silica gel column chromatography, 2,3-thiadiazoles-5-yl))-2H-1,2,4-triazole-3-ethyl thioglycolate VIII, eluent is 60～90 degrees centigrade sherwood oil: ethyl acetate, and according to the difference of compound VIII structure, volume ratio is between 10: 1～3: 1; With the pure product calculated yield of gained, yield 20-90%; Chemical structure and the physical and chemical parameter of compound VIII see Table 1.

Embodiment 8

2-replacement-(5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl))-2H-1, the synthetic and structure of 2,4-triazole-3-sulfoxide group ethyl acetate IX is identified

At ice bath with under stirring, with compound VIII 1.75 mmoles, with 10 milliliters of methylene dichloride dissolvings, add the MCPBA0.30 gram then in batches, i.e. 1.75 mmoles, react after 3 hours, concentrating under reduced pressure reaction solution behind the stopped reaction, filtrate is concentrated the back get compound 2-replacement-(5-(4-methyl isophthalic acid with 200-300 order silica gel column chromatography separating purification, 2,3-thiadiazoles-5-yl))-and 2H-1,2,4-triazole-3-sulfoxide group ethyl acetate IX, eluent are that volume ratio is 3: 1 60-90 degree centigrade sherwood oil: ethyl acetate; With the pure product calculated yield of gained, yield 20-90%; Chemical structure and the physical and chemical parameter of compound I X see Table 1.

Embodiment 9

2-replacement-(5-(4-methyl isophthalic acid, 2,3-thiadiazoles-5-yl))-2H-1, the synthetic and structure of 2,4-triazole-3-sulfuryl ethyl acetate IX is identified

At ice bath with under stirring, with compound VIII 1.75 mmoles, with 10 milliliters of methylene dichloride dissolvings, add the MCPBA0.75 gram then in batches, i.e. 4.38 mmoles, react after 3 hours, concentrating under reduced pressure reaction solution behind the stopped reaction, filtrate is concentrated the back get compound 2-replacement-(5-(4-methyl isophthalic acid with 200-300 order silica gel column chromatography separating purification, 2,3-thiadiazoles-5-yl))-and 2H-1,2,4-triazole-3-sulfuryl ethyl acetate X, eluent are that volume ratio is 3: 1 60-90 degree centigrade sherwood oil: ethyl acetate; With the pure product calculated yield of gained, yield 20-90%; Chemical structure and the physical and chemical parameter of compounds X see Table 1.

Embodiment 10

4-methyl isophthalic acid of the present invention, the antibacterial or fungicidal activity of 2,3-thiadiazoles-5-triazole class compounds I:

Title and the code name of the frequently seen plants pathogenic fungi of the present invention's test comprise AS: tomato early blight bacterium (Alternaria solani); BC: botrytis cinerea pers (Botrytis cinerea); CA: peanut Cercospora bacteria (Cercospora arachidicola); GZ: fusarium graminearum (Gibberella zeae); PI: phytophthora infestans (Phytophthora infestans (Mont.) de Bary); PP: ring rot of apple bacterium (Physalospora piricola); PS: Rhizoctonia solani Kuhn (Pellicularia sasakii); RC: cereal rhizoctonia (Rhizoctonia cerealis); SS: Sclerotinia sclerotiorum (Sclerotinia sclerotiorum), these bacterial classifications have good representativeness, can represent the kind of most of pathogenic bacteria that the field takes place in the agriculture production.Thalli growth rate method measurement result sees Table 2, table 2 shows, when 50 mcg/ml, all 4-methyl isophthalic acids that the present invention synthesizes, 2,3-thiadiazoles-5-triazole class compounds I all has fungicidal activity in various degree, and the fungicidal activity of LY3-6-20-25-1, LY3-51-3, LY3-6-19-23, the PP of LY3-7-12-43-2 is higher than 40%-60%; The fungicidal activity of LY3-6-14-17, LY2-4-11-9, LY2-4-16-10, LY3-6-9-2, LY3-6-9-1, LY3-6-8-8, LY3-6-8-10, LY3-6-20-25-1, LY3-6-8-12, LY2-5-18-44, LY3-6-19-21, LY3-51-5, LY3-6-8-7, LY3-6-19-19, LY3-7-12-43-1, the BC of LY3-7-13-44-2 is between 40%-60%; The fungicidal activity of LY2-4-11-9, LY2-5-11-40, LY3-51-7, LY3-51-6, LY3-51-10, LY3-51-9, the BC of LY3-6-8-11 is between 60%-80%; The fungicidal activity of LY3-6-20-25-1, LY3-51-10, the SS of LY3-51-9 is between 40%-60%; The fungicidal activity of LY3-6-9-1, LY4-8, LY3-51-5, LY3-6-8-7, LY3-6-19-19, LY3-51-6, LY3-7-13-45-1, LY3-51-3, the SS of LY3-7-13-44-2 is between 60%-80%; The fungicidal activity of LY3-6-9-1, LY3-51-1, the SS of LY3-7-12-43-2 is higher than 80%; The fungicidal activity of LY3-6-14-17, LY2-4-11-9, LY2-5-11-40, LY2-4-16-10, LY3-6-9-1, LY4-8, LY3-51-7, LY3-6-8-9, LY2-5-18-44, LY3-6-19-21, LY3-7-12-43-1, LY3-7-13-45-1, LY3-51-2, LY3-51-1, LY3-51-1, LY3-6-19-23, LY3-7-12-43-2, LY3-51-10, LY3-7-13-44-2, LY3-51-9, the RC of LY3-6-8-11 is between 40%-60%; The fungicidal activity of LY3-6-20-25-1, LY3-6-8-7, LY3-6-19-19, LY3-51-6, the RC of LY3-7-13-44-1 is between 60%-70%; The fungicidal activity of LY3-6-14-17, LY2-5-11-40, LY3-6-9-1, LY3-6-8-7, LY3-6-19-19, LY3-51-6, LY3-7-13-44-1, LY3-51-1, LY3-7-13-44-2, the PS of LY3-51-9 is between 40%-60%; The fungicidal activity of the PS of LY2-5-11-40 is between 60%-70%; Therefore, this compounds has shown fungicidal activity preferably.

Embodiment 11

4-methyl isophthalic acid of the present invention, the aphid activity extremely of 2,3-thiadiazoles-5-triazole class compounds I:

The present invention synthesizes the 4-methyl isophthalic acid, 2, the killing aphis determination of activity of 3-thiadiazoles-5-triazole class compounds I the results are shown in Table 3, table 3 shows when reagent agent concentration is 200 mg/litre, after the observation effect 72 hours, the poisoning rate that the poisoning rate of contrast medicine Provado and LY4-7-2 (triaxamate) reaches 100%, LY3-7-13-44-1, LY3-51-2 also reaches 96.67% and 95.16% respectively; The poisoning rate of LY2-4-16-10, LY3-7-13-45-1 is higher than 80%; The poisoning rate of LY3-51-1, LY3-51-5, LY3-51-7, LY3-51-9, LY3-51-6, LY3-6-19-21 is higher than 60%.When reagent agent concentration is 100 mg/litre, 25 mg/litre, 6.25 mg/litre, after the observation effect 48 hours: the poisoning rate of contrast medicine LY4-7-2 (triaxamate) is still near 100%, and the active of said medicine significantly reduces, and wherein has only the poisoning rate of LY3-7-13-45-1 to reach 64.29%.

Embodiment 12

4-methyl isophthalic acid of the present invention, the anti-TMV of 2,3-thiadiazoles-5-triazole class compounds VII is active:

The measurement result of TMV activity sees Table 4, and table 4 shows that majority of compounds of the present invention has the activity of anti-TMV preferably; The result for the treatment of of most compounds when 100 mcg/ml is higher than the result for the treatment of of contrast medicament TDL under the same concentrations, and wherein: the result for the treatment of of LY2-5-11-41, LY3-6-8-9, LY3-6-14-14, LY3-7-12-43-1, LY3-7-13-44-1 is higher than 44.97% of contrast medicament Ningnanmycin; The result for the treatment of of most compounds when 100 mcg/ml is higher than the protection effect of contrast medicament TDL under the same concentrations, and wherein: the protection effect of LY3-6-8-11, LY3-7-12-43-2, LY3-6-21-31, LY3-6-9-2, LY3-7-12-44-2, LY3-6-8-10, LY3-7-13-44-1 is higher than 42.01% of Ningnanmycin; The result for the treatment of of most compounds when 100 mcg/ml is higher than the inactivate activity of contrast medicament TDL under the same concentrations, and wherein: the inactivate activity of LY2-4-11-9, LY2-5-11-41, LY3-6-8-8, LY3-6-8-9 and LY3-6-9-2 is higher than 48.04% of Ningnanmycin; The induced activity of LY3-6-19-21 when 100 mcg/ml is higher than contrast medicament TDL.Therefore, this compounds has shown the activity of general anti-plant tobacco mosaic virus.

Embodiment 13

4-methyl isophthalic acid of the present invention, the application in 2,3-thiadiazoles-5-triazole class compounds I and sterilant combination control agricultural and forestry and the gardening plant insect pest

All 4-methyl isophthalic acids of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and existing sterilant: Chlorpyrifos 94, the inferior Nong in ground, acetamiprid, Affirm (Merck Co.), more visit rhzomorph, Avrmectin, pleocidin, fenvalerate, efficient fenvalerate, Cypermethrin, effective cypermethrin, lambda-cyhalothrin, Deltamethrin, Fenvalerate, the Beta-cyfloxylate, cyfloxylate, the Lambda-lambda-cyhalothrin, Permanone, permethrin, esbiothrin, cyhalothrin, bifenthrin, permethrin, ether chrysanthemum ester, flumethrin, fluvalinate, Provado, acetamiprid, Ti304, imidaclothiz, thiophene worm quinoline, thiophene worm piperazine, thiophene worm amine, MTI-446, clothianadin, Da Tenan, diflubenzuron, young urea goes out, Teflubenzuron, deinsectization is grand, fluorine bell urea, flufenoxuron, the pyridine worm is grand, the Acarus tritici urea, the poisonous insect urea, penfluron, Noviflumuron is noviflumuron, and its CAS number is 121451-02-3, flucycloxuron, Novaluron is Rimon, fluorine pyridine urea, Bay sir6874 i.e. { 1-[(3.5-two chloro-4) 4-nitrophenoxy phenyl 3-3-(2-chlorobenzene)-urea }, Bay SIR-8514 i.e. [1-(4-Trifluoromethoxyphen-l)-3-(2-chlorobenzene)-urea], piperazine worm urea, namely two three flufenoxuron of Bistrifluron, furans worm hydrazides, the worm hydrazides, chlorine worm hydrazides, methoxyfenozide, ring worm hydrazides, Rogor, omethoate, SD-1750, acephate, triazophos, Resitox, pyridaphenthione, isazofos, Ro 7-5050, SevinCarbaryl, Aphox, meta-tolyl-N-methylcarbamate (MTMC), isoprocarb, cartap, fenobucarb, leaf disperses, carbaryl, benfuracarb, carbosulfan, cartap, bromopropylate, hexythiazox, azoles mite ester, pyridaben, four mite piperazines, alkynes mite spy, the butyl ether urea, benfuracarb, pyrrole aphid ketone, spiral shell mite ester, spiral shell worm ester, spiral shell worm ethyl ester, butene-fipronil, azocyclotin, Buprofezin, ethoprophos, fluorine worm nitrile, the desinsection list, disosultap, the chlorine insect amide, Flubendiamide, the fluorine cyanogen insect amide, cyanogen insect amide, Tolfenpyrad, tebufenpyrad, bromothalonil, pyrazine ketone, second mite azoles, tebufenpyrad, the young ketone of rattling away, the pyrrole propyl ether, in the emaricin etc. any one or two kinds are used in combination for control agricultural and forestry and gardening plant insect pest; 4-methyl isophthalic acid of the present invention, 2, the 3-thiadiazoles-quality percentage composition of 5-triazole class compounds I in composition is 1%-90%, 4-methyl isophthalic acid of the present invention, the ratio of 2,3-thiadiazoles-5-triazole class compounds I and above-mentioned sterilant is mass percent 1%: 99% to 99%: 1%; Spray after can directly converting water, comprise agricultural in the preparation of composition and go up acceptable solvent and emulsifying agent and solubility promoter and synergistic agent etc., the formulation of composition processing is selected from sustained release dosage, pulvis, micro-capsule suspension, the dispersible body preparation, the dispersible solid preparation, seed treatment emulsion, aqueous emulsion, granule, microemulsion, finish, seed with coated pesticidal, suspended emulsion agent, soluble thick agent, poison grain, aerosol, block poison bait, sustained-release block, dense poison bait, capsule suspension, can disperse dense dose, missible oil, the electrostatic spray agent, water-in-oil emulsion, seed treatment agent, oil-in-water emulsion, smoke candle, granula subtilis, smoke candle, smoke cartridge, the smog rod, the smog sheet, smoke substance, the smog ball, granular poison bait, foaming agent, ointment, thermal fog, solid-liquid mixes the dress agent, liquid/liquid mixes the dress agent, cold mist agent, Gu Gu/mix and adorn agent, the medicine lacquer, the seed treatment liquor, microgranules, oil suspending agent, finish, the oil-dispersing property pulvis, paste, the sheet poison bait, dense jelly, sprinkle and water agent, stylus, plant the clothing agent, poison bait, basting agent, the fritter poison bait, suspension agent, suspension emulsion, water-soluble granule, soluble thick agent, the film forming finish, tablet, follow the trail of pulvis, ultra low volume liquids, in the steam releasing agent any one; The insect pest that can prevent and treat mainly contains red spider, Asiatic migrotory locust, clouding car locust, Chinese rice grasshopper, Patanga japonica (l.Bol.), single thorn mole cricket, the east mole cricket, rice thrips, onion thrips, greenhouse thrips, haplothrips aculeatus, Mai Jian manages thrips, Trialeurodes vaporariorum Westwood, Bemisia tabaci, rice green leafhopper, green leaf hopper, chlorita biguttula, spot clothing plant hopper, brown paddy plant hopper, white backed planthopper, small brown rice planthopper, the flat angle of sugarcane plant hopper, cotten aphid, green bugs, grain aphid, black peach aphid, kaoliang aphid, radish aphid, icerya purchasi, Pseudaulacaspis pentagona, unaspis shield kuwana, san jose scale, wax insect, ceroplastes rubens, the hard a red-spotted lizard of Korea's ball, pear lace bug, the banana lace bug, thin corner piece stinkbug, little minute pirate bugs, slender rice bug, paddy fly, niphe elongata, scotinophora lurida, Nezara viridula smaragdula Fabricius., green plant bug, alfalfa plant bug, black striped plant bug, chrysopa septempunctata, beautiful Chrysopa, Chinese green lacewing, rain moth, casemaking clothes moth, cnidocampa flavescens walker, brown slug moth, thosea siensis, gelechiid, pink bollworm, brachmia triannuella, small cabbage moth, small heart-eating peach worm, eating-core bean worm, small heart-eating peach worm, the apple Spilonota lechriaspis, brown belt length leaf roller, intend smaller apple leaf roller, striped rice borer, bean-pod borer, Pyrausta nubilalis (Hubern)., yellow rice borer, Oeobia undalis, Cnaphalocrocis medinali(rice leaf roller), the bar snout moth's larva, the wild snout moth's larva of lap leaf, dichocrocis punctiferalis, armyworm, prodenia litura, rice green caterpillar, anomis flava, beet armyworm, pink rice borer, bollworm, ancient cooking vessel point diamond drill, black cutworm, big cutworm, yellow cutworm, steal poison moth, gypsymoth, palaearctic sweet potato, greenish brown hawk moth, the straight burr rice hesperiidae, pelopidas mathias, the oranges and tangerines swallowtail butterfly, Common Mormon, small white, pyrameis indica, the yellow a kind of butterfly harmful to crop plants of ramie, the beans blister beetle, the Venus ground beetle, wrinkle sheath ground beetle, wheat head ground beetle, pleonomus canaliculatus, Agriotes subrittatus Motschulsky, khapra beetle, attagenus piceus, the little buprestid beetle of oranges and tangerines, gold edge buprestid beetle, tenebrio molitor, dark mealworm, red flour beetle, confused flour beetle, the verdigris different beetle, black dull cockchafer, holotrichia oblita, mulberry borer, longicorn beetle, nadezhdiella cantori, pink neck longicorn, big daikon leaf beetle, daicon leaf beetle, aulacophora femoralis, Phyllotreta striolata, Callosobruchus chinensis, pea weevil, broad bean weevil, sitophilus zea-mais, rice weevil, dolerus tritici, pear fruit sawfly, the yellowish leukorrhea ichneumon wasp, armyworm white star ichneumon wasp, corn earworm is hanged the cocoon ichneumon wasp, bollworm tooth lip ichneumon wasp, snout moth's larva stain wart ichneumon wasp, mosquito, fly, horsefly, wheat midge, contarinia tritici, pachydiplosis oryzae, citrus fruit fly, the melon trypetid, the latent fly of wheat leaf ash, Americal rice leaf miner, the black fly of diving of beans stalk, frit fly, plant fly, onion fly, the radish fly, full skirt chases after posts fly, Pyrausta nubilalis (Hubern). is strict posts fly, armyworm lacks Agricultural pests such as must posting fly, forestry pest; Plant in control agricultural and forestry and the gardening plant insect pest comprises paddy, wheat, barley, oat, corn, Chinese sorghum, sweet potato, potato, cassava, soybean, pea-pods, broad bean, pea, mung bean, red bean, cotton, silkworm and mulberry, peanut, rape, sesame, Sunflower Receptacle, beet, sugarcane, coffee, cocoa, genseng, the bulb of fritillary, rubber, coconut, oil palm, sisal hemp, tobacco, tomato, capsicum, radish, cucumber, Chinese cabbage, celery, hot pickled mustard tube, beet, rape, green onion, garlic, watermelon, muskmelon, hami melon, pawpaw, really, tea, wild vegetable, bamboo shoots, hops, paddy rice, pepper, apple, banana, citrus, peach, papaya, orchid, potted landscape.Composition has improved the defence capability of plant in desinsection, make plant produce defence capability to pathogenic fungi, bacterium and virus infection.

Embodiment 14

4-methyl isophthalic acid of the present invention, the application in 2,3-thiadiazoles-5-triazole class compounds I and miticide combination control agricultural and forestry and the gardening plant mite evil

4-methyl isophthalic acid of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and agricultural go up acceptable assistant and be selected from azocyclotin, cyhexatin, fenbutatin oxide, three phosphor tins, Zaprawa enolofos, dimethylvinphos, crotoxyphos, SD-1750, heptenopos, Phosdrin, monocrotophos, naled, Chlorpyrifos 94, Pyrimithate, imino-formyl chloride sulphur phosphorus, omethoate, dioxathion, Nialate, the Malathion, methacrifos, Phosalone, Volaton, methylpyrimidine sulphur phosphorus, Resitox, sulfotep, triazophos, vamidothion, isocarbophos, acephatemet, propetamphos, dialifos, R-1504, acrinathrin, bifenthrin, cyhalothrin, smart lambda-cyhalothrin, Fenvalerate, flucythrinate, flumethrin, taufluvalinate, brofluthrinate, Bifenazate, fenothiocarb, aldicarb, butocarboxim, oxamyl, Talcord, thiofanox, F-1991, sok, carbofuran, carbosulfan, meta-tolyl-N-methylcarbamate (MTMC), promacyl, formetanate, single carbonamidine, medimeform, amitraz, chlordimeform, peruscabin, bromopropylate, fourth fluorine mite ester, the mite quinone goes out, Nissol, flufenoxuron, macro tetrolide, piericidin, thuringiensin, tetranactin, macro tetrolide, Avrmectin, doractin, the Ai Pulinuo rhzomorph, ivermectin, rhzomorph is drawn in match, moxidectin, pyrethrin, nicotine, matrine, nimbin, tubatoxin, tebufenpyrad, pyridaben, azoles mite ester, four mite piperazines, alkynes mite spy, hexythiazox, spiral shell mite ester, Fluacrypyrim, Ovotran, propargite, in the pyridaben any one or two kinds of medicament combined preparation become miticide to be used for control agricultural and forestry and gardening plant mite evil; 4-methyl isophthalic acid of the present invention, the total quality percentage composition of 2,3-thiadiazoles-5-triazole class compounds I in composition is 1%-90%, 4-methyl isophthalic acid of the present invention, the ratio of 2,3-thiadiazoles-5-triazole class compounds I and above-mentioned medicament is mass percent 1%: 99% to 99%: 1%; The formulation of composition processing is selected from sustained release dosage, pulvis, micro-capsule suspension, the dispersible body preparation, the dispersible solid preparation, seed treatment emulsion, aqueous emulsion, granule, microemulsion, finish, seed with coated pesticidal, suspended emulsion agent, soluble thick agent, poison grain, aerosol, block poison bait, sustained-release block, dense poison bait, capsule suspension, can disperse dense dose, missible oil, the electrostatic spray agent, water-in-oil emulsion, seed treatment agent, oil-in-water emulsion, smoke candle, granula subtilis, smoke candle, smoke cartridge, the smog rod, the smog sheet, smoke substance, the smog ball, granular poison bait, foaming agent, ointment, thermal fog, solid-liquid mixes the dress agent, liquid/liquid mixes the dress agent, cold mist agent, Gu Gu/mix and adorn agent, the medicine lacquer, the seed treatment liquor, microgranules, oil suspending agent, finish, the oil-dispersing property pulvis, paste, the sheet poison bait, dense jelly, sprinkle and water agent, stylus, plant the clothing agent, poison bait, basting agent, the fritter poison bait, suspension agent, suspension emulsion, water-soluble granule, soluble thick agent, the film forming finish, tablet, follow the trail of pulvis, ultra low volume liquids, in the steam releasing agent any one; Plant in composition for preventing and controlling agricultural and forestry and the gardening plant mite evil is selected from paddy, wheat, barley, oat, corn, Chinese sorghum, sweet potato, potato, cassava, soybean, pea-pods, broad bean, pea, mung bean, red bean, cotton, silkworm and mulberry, peanut, rape, sesame, Sunflower Receptacle, beet, sugarcane, coffee, cocoa, genseng, the bulb of fritillary, rubber, coconut, oil palm, sisal hemp, tobacco, tomato, capsicum, radish, cucumber, Chinese cabbage, celery, hot pickled mustard tube, beet, rape, green onion, garlic, watermelon, muskmelon, hami melon, pawpaw, really, tea, wild vegetable, bamboo shoots, hops, potato, paddy rice, pepper, apple, banana, citrus, peach, papaya, orchid, potted landscape; The mite evil that composition is suitable for is phytophagy evil mite, and it is that the harmful mite of Tetranychidae, Tenuipalpidae, furan line mite, Eriophyidae is that Panonychus citri belongs to, tetranychus telarius belongs to and these global agricultural evil mites of the itch mite of Eriophyidae, forestry evil mite, the harmful mite of gardening and the harmful mite of health that phytophagy evil mite is selected from tetranychid.

Embodiment 15

4-methyl isophthalic acid of the present invention, the application in 2,3-thiadiazoles-5-triazole class compounds I and sterilant combination control agricultural and forestry and the gardening plant disease

all 4-methyl isophthalic acids of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and existing bactericide such as diazosulfide, tiadinil, be abbreviated as TDL, tisocromide, the first thiophene lures amine, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-formic acid, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-sodium formate, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-Ethyl formate, the DL-beta-aminobutyric acid, isotianil, it is English general by name: isotianil, 3,4-, two chloroisothiazoles-5-formic acid, 3,4-, two chloroisothiazoles-5-sodium formate, 3,4-, two chloroisothiazoles-5-Ethyl formate, virazole, antofine, Ningnanmycin or salicylic acid, frost urea cyanogen, thiram, ziram, Mancozeb, aliette, thiophanate-methyl, Bravo, the enemy can be loose, procymidone, fenpropidin, thiophanate methyl, thiophanate, Metalaxyl-M, flumorph, dimethomorph, efficient metalaxyl, efficient M 9834, two chlorine zarilamids, flusulfamide, the first flusulfamide, thiophene fluorine bacterium amine, flutolanil, tecloftalam, ring propionyl bacterium amine, cyflufenamid, fenhexamid, zarilamid, Silthiopham, furametpyr, the pyrrole metsulfovax, mandipropamid, zoxamide, fenfuram, carboxin, chlozolinate, iprodione, Fluoxastrobin, dimoxystrobin, fluoxastrobin, kresoxim-methyl, SSF 126, orysastrobin, ZEN 90160, pyraclostrobin, oxime bacterium ester, Enestroburin, alkene oxime amine, oxygen ring azoles, bromuconazole, Cyproconazole, Difenoconazole, alkene azoles alcohol, efficient alkene azoles alcohol, epoxiconazole, RH-7592, Fluquinconazole, Flusilazole, Flutriafol, own azoles alcohol, glyoxalin, plant the bacterium azoles, metconazole, nitrile bacterium azoles, penconazole, propiconazole, prothioconazoles, simeconazoles, Tebuconazole, tetraconazole, Triadimenol, triticonazole, bitertanol, probenazole, furidazol, imazalil, efficient imazalil, Prochloraz, fluorine bacterium azoles, cyazofamid, Fenamidone, the Evil imidazoles, pefurazoate, famoxadone, SYP-Z048, hymexazo, the spirit of Evil frost, Guardian, Grandox fumigant, octhilinone, benthiozole, dodemorph, butadiene morpholine, tridemorph, fenpiclonil, fludioxonil, fluazinam, pyrifenox, ring pyridine bacterium amine, Boscalid, fluopicolide, pyridine bacterium amine, cyprodinil, the fluorine mepanipyrim, ferimzone, mepanipyrim, phonetic mould amine, Fenarimol, nuarimol, chinomethionat, dithianon, ethoxyquin, oxyquinoline, the third oxygen quinoline, benzene oxygen quinoline, the mould prestige of second, iprovalicarb, the benzene metsulfovax, Propamocarb, methasulfocarb, edifenphos, IBP, pyrazophos, tolelofos-methyl, blasticidin-S, kasugarnycin, polyoxin, Polyoxin, valida, jinggangmeisu, streptomysin, metalaxyl, furalaxyl, M 9834, ofurace, mebenil, carbendazim, benomyl, thiophanate-methyl, triazolone, bupirimate, dimethirimol, the phonetic phenol of second, difoltan, captan, folpet, vinclozolin, fluoromide, dimethachlon, Bravo, Isoprothiolane, kitazine, Yekuzuo, pentachloronitrobenzene, Propineb, phosethyl-Al, sulphur, Bordeaux mixture, copper sulphate, copper oxychloride, cuprous oxide, Kocide SD, metrafenone, Pencycuron, diclomezin, Rabcide, pyroquilon, volution bacterium amine, tricyclazole, triforine, the pyridine of many fruits, the hot salt of biguanides, iminoctadine, botran, the benzene flusulfamide, the toluene flusulfamide, K-281, fenaminosulf, oxolinic acide, probenazole, bronopol, iodomethane, metham-sodium, enemy's line ester, dazomet, nemamort, lythidathion, cadusafos, fensulfothion, thionazin, fenamiphos, phonamiphos, dichlofenthion, isazofos, fosthietan, oxamyl, Aldicarb, carbofuran, vikane, dichloropropylene, dichloro-isonicotinic acid, other known any any one or two kinds that can be used as in bactericide such as allyl isothiazole are used in combination for control agricultural and forestry and gardening plant disease, 4-methyl isophthalic acid of the present invention, the total quality percentage composition of 2,3-thiadiazoles-5-triazole class compounds I in composition is 1%-90%, 4-methyl isophthalic acid of the present invention, the ratio of 2,3-thiadiazoles-5-triazole class compounds I and aforementioned bactericide is mass percent 1%: 99% to 99%: 1%, the prevention effect of composition is good, and these compositions have certain synergistic effect and summation action, does not find to have the composition of antagonistic action, above-mentioned composition can be used for the control of agricultural plant disease and gardening plant disease, controlling object comprises that more than 20 of the Achylas, Aphanomyces, pythium, Phytophthora, Sclerospora, Plasmopara, Pseudoperonospora, Peronospora of Oomycete etc. belong to the diseases that produce, as other diseases of plurality of cereals crop, industrial crops, gardening plant and the forestry plants such as seedling blight of rice, tomato root maize ear rot, the late blight of potato, black shank, millet powdery mildew, downy mildew of garpe, downy mildew of lettuce, cucumber downy mildew, cucumber anthracnose etc., the formulation of composition processing is selected from sustained release agent, pulvis, micro-capsule suspension, the dispersible body preparation, the dispersible solid preparation, seed treatment emulsion, aqueous emulsion, granule, microemulsion, finish, seed with coated pesticidal, suspension emulsion, soluble thick agent, poison grain, aerosol, block poison bait, sustained-release block, dense poison bait, capsule suspension, can disperse dense dose, missible oil, the electrostatic spray agent, water-in-oil emulsion, seed treatment, oil in water emulsion, smoke candle, granula subtilis, smoke candle, smoke cartridge, the smog rod, the smog sheet, smoke agent, the smog ball, granular poison bait, foaming agent, ointment, thermal fog, solid-liquid mixes the dress agent, liquid/liquid mixes the dress agent, cold mist agent, Gu Gu/mix filling agent, the medicine paint, the seed treatment liquor, fine granule, oil suspending agent, finish, the oil-dispersing property pulvis, paste, the sheet poison bait, dense jelly, sprinkle and water agent, stylus, seed coat agent, poison bait, liniment, the fritter poison bait, suspending agent, suspended emulsion, water-soluble granule, soluble thick agent, the film forming finish, tablet, follow the trail of pulvis, ultra low volume liquids, any one in the steam releasing agent.These compositions are used for control agricultural and forestry and the suitable plant of gardening plant disease and comprise cereal: paddy, wheat, barley, oat, corn, millet, Chinese sorghum; Tuber crops: sweet potato, potato, cassava; Beans: soybean, broad bean, pea, mung bean, red bean and fiber: cotton, crudefiber crop, silkworm and mulberry; Oil plant: peanut, rape, sesame, soybean, Sunflower Receptacle; Sugar material: beet, sugarcane; Beverage: tealeaves, coffee, cocoa; Hobby: tobacco leaf; Medicinal: genseng, the bulb of fritillary; The torrid zone: rubber, coconut, oil palm, sisal hemp; Food crop and fruit, flowers, oil plant, sugar material and cotton, fiber crops, tea, tobacco, Chinese medicinal materials cash crop and plant melon, really, tea, silkworm and mulberry, vegetables, contain various wild vegetable, bamboo shoots, flowers and ornamental plant, hops, medicinal material, pepper, seedling and other garden crops such as tobacco: flue-cured tobacco, air-curing of tobacco leaves, suncured tabacco; Vegetables, tomato, capsicum, radish, cucumber, Chinese cabbage, celery, hot pickled mustard tube, beet, rape, green onion, garlic, melon: watermelon, muskmelon, hami melon, pawpaw; Beans: soybean, broad bean, pea-pods; Potato, wheat, corn, paddy rice, peanut, fruit tree: apple, banana, citrus, peach, papaya; Flowers: orchid; Potted landscape; Composition has improved the defence capability of plant in sterilization, make plant produce defence capability to pathogenic fungi, bacterium and virus infection.

Embodiment 16

4-methyl isophthalic acid of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and antiviral agent are combined in the application in control agricultural and forestry and the gardening plant virus disease

4-methyl isophthalic acid of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and existing Antiphytoviral medicament diazosulfide, tiadinil, be abbreviated as TDL, different metsulfovax, it is English general by name: isotianil, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-formic acid, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-sodium formiate, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-ethyl formate, 3,4-two chloroisothiazoles-5-formic acid, 3,4-, two chloroisothiazoles-5-sodium formiate, 3,4-, two chloroisothiazoles-5-ethyl formate, the DL-beta-aminobutyric acid, virazole, antofine, Ningnanmycin, tisocromide, the first thiophene lures amine or Whitfield's ointment, cytosintetidemycin, dichloro-isonicotinic acid, allyl isothiazole, well ridge azanol, any 1 or the combination of 2 compounds are used for control agricultural and forestry and gardening plant virus disease in the jingganmycin; The disease of control agricultural and forestry and gardening plant virus disease is selected from tobacco mosaic virus disease, various melon virus diseases, various solanberry viroid diseases, the beans virus disease, the Cruciferae virus disease, the grain and oil crop virus disease, any in cotton virus disease and the various fruit tree virus disease, wherein endanger serious being selected from: tobacco virus, peppery pimento virus disease, tomato virus disease, Chinese cabbage virus disease, the paddy rice virus disease comprises rice dwarf virus disease, yellow dwart, stripe virus disease, the fern leaf of tomato viral disease, sick and the tobacco veinal necrosis virus disease of chilli pepper mosaic virus, the corn short mosaic disease, cauliflower mosaic virus, the oranges and tangerines virus disease, cymbidium mosaic virus, any in the cybidium ring spot virus.The plant that these compositions are used for control agricultural and forestry and gardening plant virus disease is selected from paddy, wheat, barley, oat, corn, Chinese sorghum, sweet potato, potato, cassava, soybean, pea-pods, broad bean, pea, mung bean, red bean, cotton, silkworm and mulberry, peanut, rape, sesame, Sunflower Receptacle, beet, sugarcane, coffee, cocoa, genseng, the bulb of fritillary, rubber, coconut, oil palm, sisal hemp, tobacco, tomato, capsicum, radish, cucumber, Chinese cabbage, celery, hot pickled mustard tube, beet, rape, green onion, garlic, watermelon, muskmelon, hami melon, pawpaw, really, tea, wild vegetable, bamboo shoots, hops, potato, paddy rice, pepper, apple, banana, citrus, peach, papaya, orchid, agriculturals such as potted landscape, gardening, economical, plants such as forestry; The use of these compositions makes the immunizing power of crop self improve, and has induced the defence capability of plant generation to viral diseases of plants when producing the control of insect especially infection insect; Also can produce the direct prevention effect of virus disease; Therefore, these compositions can be used for Antiphytoviral medicament and inducing plant Antiphytoviral medicaments preparation and purposes.4-methyl isophthalic acid of the present invention, 2, the total quality percentage composition of 3-thiadiazoles-5-triazole class compounds I in composition is 1%-90%, 4-methyl isophthalic acid of the present invention, the ratio of 2,3-thiadiazoles-5-triazole class compounds I and aforementioned Antiphytoviral medicament is mass percent 1%: 99% to 99%: 1%; The formulation of composition processing is selected from sustained release dosage, pulvis, micro-capsule suspension, the dispersible body preparation, the dispersible solid preparation, seed treatment emulsion, aqueous emulsion, granule, microemulsion, finish, seed with coated pesticidal, suspended emulsion agent, soluble thick agent, poison grain, aerosol, block poison bait, sustained-release block, dense poison bait, capsule suspension, can disperse dense dose, missible oil, the electrostatic spray agent, water-in-oil emulsion, seed treatment agent, oil-in-water emulsion, smoke candle, granula subtilis, smoke candle, smoke cartridge, the smog rod, the smog sheet, smoke substance, the smog ball, granular poison bait, foaming agent, ointment, thermal fog, solid-liquid mixes the dress agent, liquid/liquid mixes the dress agent, cold mist agent, Gu Gu/mix and adorn agent, the medicine lacquer, the seed treatment liquor, microgranules, oil suspending agent, finish, the oil-dispersing property pulvis, paste, the sheet poison bait, dense jelly, sprinkle and water agent, stylus, plant the clothing agent, poison bait, basting agent, the fritter poison bait, suspension agent, suspension emulsion, water-soluble granule, soluble thick agent, the film forming finish, tablet, follow the trail of pulvis, ultra low volume liquids, in the steam releasing agent any one; All show addition or synergism between these compositions, when keeping insecticidal activity, the effect that its antiviral activity all uses separately greater than any one compound; Find no the composition of antagonistic action, the drug effect lasting period of composition is long.

Embodiment 17

4-methyl isophthalic acid of the present invention, complete processing and the stability of 2,3-thiadiazoles-5-triazole class compounds I and commercially available agricultural chemical compound preparation

4-methyl isophthalic acid of the present invention, 2, the mixed preparation complete processing of 3-thiadiazoles-5-triazole class compounds I and commercially available agricultural chemical sees Table 5, by table 5 as seen, most medicament all can be processed according to the method for statement, the main component of liquid preparation is effective constituent and solubility promoter and tensio-active agent, synergistic agent, antifreezing agent, stablizer, other component etc. such as thickening material or permeate agent, the composition of solid preparation mainly includes the effect composition, other agriculturals such as tensio-active agent and filler go up the acceptable adjuvant component, the cold storage test of process preparation, liquid preparation is placed 1 week not have to precipitate at 0 ± 2 degree centigrade and is separated out, solid preparation placed for 2 weeks at 54 ± 2 degrees centigrade, caking phenomenon does not appear in medicament, the medicament drug effect that all preparations store before and after placing does not have significant difference, the rate of decomposition of composition effective constituent in 5%, the composite preparation qualified stability.Commercially available agricultural chemical of the present invention is aforesaid sterilant, miticide, sterilant, anti-plant virus agent.

Table 2 4-methyl isophthalic acid of the present invention, the bacteriostatic activity of 2,3-thiadiazoles-5-triazole class compounds I (/ %)

Compound	AS	CA	GZ	PP	BC	SS	RC	PS	PI
										LY4-8	19.35	15.38	5.56	36.73	34.04	79.31	50.79	33.33	13.16
LY2-4-11-9	12.90	3.85	0	3.77	67.50	16.67	52.78	22.62	12.50
										LY2-5-11-40	20.59	15.38	18.92	50.00	62.50	21.62	54.24	63.10	18.18
LY2-4-16-10	17.65	19.23	37.84	34.78	52.50	21.62	55.93	22.62	12.12
										LY3-6-9-2	12.90	7.69	6.00	22.64	50.00	23.33	20.83	8.33	15.00
LY3-6-9-1	12.90	7.69	10.00	24.39	52.00	82.35	55.71	50.00	17.14
										LY3-51-7	14.71	7.69	21.62	36.96	75.00	24.32	45.76	42.86	12.12
LY3-6-8-8	19.35	15.38	2.00	32.08	45.00	23.33	37.50	25.00	32.50
										LY3-6-21-31	9.68	11.54	0	9.43	25.00	3.33	34.72	16.67	10.00
LY3-6-14-14	9.68	11.54	2.00	24.53	32.50	26.67	47.22	22.62	32.50
										LY3-6-8-10	16.13	11.54	4.00	20.75	45.00	26.67	54.17	36.90	25.00
LY3-6-20-25-1	29.03	15.38	22.50	48.78	50.00	50.00	67.14	54.76	31.43
										LY3-6-8-12	25.81	11.54	8.00	10.00	55.00	0.00	34.72	16.67	17.50
LY3-6-14-17	12.90	3.85	8.00	9.43	47.50	20.00	51.39	45.24	20.00
										LY3-6-8-9	6.45	3.85	6.00	30.19	25.00	36.67	50.00	51.19	12.50
LY2-5-18-44	12.90	11.54	6.00	28.30	45.00	16.67	56.94	7.14	20.00
										LY3-6-19-21	22.58	15.38	24.00	30.19	55.00	23.33	55.56	8.33	27.50
LY3-51-5	17.65	7.69	8.11	28.26	52.50	62.16	42.37	30.95	12.12
										LY3-6-8-7	25.81	7.69	25.00	12.20	40.00	79.41	60.00	53.57	31.43
LY3-6-19-19	16.13	19.23	20.00	34.15	48.00	76.47	64.29	48.81	25.71
										LY3-7-12-43-1	20.59	15.38	16.22	34.78	57.50	81.08	50.85	38.10	18.18
LY3-51-6	32.26	23.08	15.00	17.07	60.00	76.47	62.86	51.19	31.43
										LY3-7-13-44-1	12.90	32.26	2.00	18.87	35.00	30.00	61.11	57.14	32.50
LY3-7-13-45-1	12.90	11.54	7.50	21.95	34.00	79.41	48.57	33.33	11.43
										LY3-51-2	9.68	11.54	5.56	36.73	27.66	20.69	47.62	4.76	7.89
LY3-51-3	12.90	7.69	16.67	40.82	31.91	79.31	39.68	25.00	26.32
										LY3-51-1	12.90	7.69	16.67	24.49	34.04	86.21	57.14	48.81	23.68
LY3-6-19-23	12.90	19.23	22.22	42.86	27.66	31.03	57.14	22.62	15.79
										LY3-7-12-43-2	12.90	11.54	16.67	44.90	42.55	82.76	42.86	11.90	15.79
LY3-51-10	20.59	3.85	18.92	30.43	70.00	51.35	40.68	27.38	3.03
										LY3-7-13-44-2	16.13	15.38	15.00	31.71	40.00	76.47	58.57	57.14	25.71
LY3-51-9	20.59	11.54	27.03	32.61	60.00	56.76	49.15	44.05	18.18
										LY3-51-8	11.23	13.43	17.54	30.12	34.09	20.47	34.01	27.09	19.01
LY3-7-15-49-2	18.34	12.02	13.09	30.01	36.00	31.01	34.08	27.01	23.09
										LY3-51-4	17.92	7.98	20.76	38.01	38.00	39.34	42.89	23.09	18.13
LY3-6-8-11	12.90	11.54	10.00	18.87	62.50	3.33	52.78	5.95	15.00
										Aphid azoles prestige	25.81	11.54	8.00	35.85	45.00	10.00	45.83	4.76	30.00

Data are the measurement result of 50 mcg/ml; AS: tomato early blight bacterium (Alternaria solani); BC: botrytis cinerea pers (Botrytis cinerea); CA: peanut Cercospora bacteria (Cercospora arachidicola); GZ: fusarium graminearum (Gibberella zeae); PI: phytophthora infestans (Phytophthora infestans (Mont.) de Bary); PP: ring rot of apple bacterium (Physalospora piricola); PS: Rhizoctonia solani Kuhn (Pellicularia sasakii); RC: cereal rhizoctonia (Rhizoctonia cerealis); SS: Sclerotinia sclerotiorum (Sclerotinia sclerotiorum).

The 4-methyl isophthalic acid that table 3 the present invention synthesizes, the The selection result of 2,3-thiadiazoles-aphid of 5-triazole class compounds I

Annotate: ND represents undetermined

The 4-methyl isophthalic acid that table 4 the present invention synthesizes, and the antiviral activity of 2,3-thiadiazoles-5-triazole class compounds I (inhibiting rate/%)

Compound	The concentration mg/litre	Therapeutic activity	Protection is active	Inactivate activity	Induced activity
						LY4-8	100	32.52±6.14	16.86±5.19	11.54±5.88	39.14±4.08
LY2-4-11-9	100	28.57±4.76	49.51±3.06	35.62±2.74	12.96±3.50
						LY2-5-11-40	100	38.62±3.72	10.35±5.26	23.81±.19	29.84±3.55
LY2-4-16-10	100	14.81±6.41	33.33±3.70	27.86±4.19	14.82±3.50
						LY3-6-9-2	100	33.86±4.00	50.49±2.25	46.12±3.45	21.76±4.24
LY3-6-9-1	100	35.77±4.28	34.48±4.60	13.49±5.37	32.56±4.19
						LY3-51-7	100	45.53±1.86	16.47±4.79	32.14±3.57	9.30±4.19
LY3-6-8-8	100	40.21±4.85	48.04±3.70	16.90±4.19	25.00±4.17
						LY3-6-21-31	100	12.70±4.20	36.76±4.42	45.21±5.97	22.22±4.17
LY3-6-14-14	100	51.85±3.31	40.69±3.70	22.38±2.85	19.44±4.17
						LY3-6-8-10	100	11.64±4.85	30.39±5.94	42.01±3.45	23.61±3.68
LY3-6-20-25-1	100	9.00±3.30	16.67±2.25	24.66±6.28	19.91±4.88
						LY3-6-8-12	100	31.75±4.77	32.35±1.47	15.07±4.11	18.52±5.61
LY3-6-14-17	100	30.69±6.61	33.33±5.17	16.44±3.62	24.54±2.89
						LY3-6-8-9	100	51.85±4.00	53.43±4.49	21.01±6.18	20.83±3.67
LY2-5-18-44	100	23.28±2.43	38.73±2.25	30.14±4.94	16.67±2.78
						LY3-6-19-21	100	11.64±3.99	24.02±2.25	34.25±4.94	34.26±2.89
LY3-51-5	100	41.87±3.73	20.69±3.04	19.84±5.87	10.85±7.01
						LY3-6-8-7	100	24.45±4.22	19.67±2.33	25.76±2.44	15.56±3.43
LY3-6-19-19	100	27.51±4.85	17.16±2.25	27.40±4.94	16.67±5.01
						LY3-7-12-43-1	100	46.03±5.72	33.33±5.17	37.90±4.81	15.74±2.89
LY3-51-6	100	16.26±4.93	18.39±7.54	8.33±4.29	8.91±4.08
						LY3-7-13-44-1	100	50.79±5.72	15.20±4.50	47.49±4.18	15.28±3.67
LY3-7-13-45-1	100	24.87±3.30	34.31±3.70	33.79±4.81	21.29±2.12
						LY3-51-2	100	27.32±3.50	11.54±5.88	23.00±4.51	27.19±4.23
LY3-51-3	100	23.58±4.93	15.32±5.19	14.68±4.81	36.82±4.08
						LY3-51-1	100	45.12±5.32	18.77±4.04	18.65±4.81	44.57±3.55
LY3-6-19-23	100	34.55±5.50	21.84±3.45	14.68±4.96	18.60±6.98
						LY3-7-12-43-2	100	40.74±3.30	34.80±6.12	46.12±4.18	25.00±3.68
LY3-51-10	100	37.40±5.50	26.82±6.33	10.71±5.46	34.88±4.65
						LY3-7-13-44-2	100	36.51±3.18	43.63±3.70	51.60±4.81	25.00±3.68
LY3-51-9	100	29.27±5.59	31.80±5.18	40.08±3.64	51.55±1.78
						LY3-51-8	100	34.00+4.33	24.06+3.44	32.09±4.01	12.43±4.76
LY3-7-15-49-2	100	24.87±6.42	31.37±6.95	28.77±5.97	14.81±8.37
						LY3-51-4	100	43.09±4.93	17.24±4.60	12.70±5.37	34.50±3.55
LY3-6-8-11	100	10.05±2.42	24.02±2.25	44.75±3.45	28.70±2.89
						Ningnanmycin	100	44.97±4.00	48.04±3.70	42.01±3.45	20.37±2.89
TDL	100	13.23±4.85	22.06±5.30	26.94±5.70	30.09±3.49

The 4-methyl isophthalic acid that table 5 the present invention synthesizes, the working method that 2,3-thiadiazoles-5-triazole class compounds I and commercially available agricultural chemical are used with

Claims

1. a class 4-methyl isophthalic acid, 2,3-thiadiazoles-5-triazole class compounds is characterized in that having the chemical structure of general formula suc as formula shown in the I:

The 4-methyl isophthalic acid of formula I, 2,3-thiadiazoles-5-triazole class compounds are specially V, VI, VII, VIII, IX, X6 kind form:

In the said structure general formula: RCO is selected from: N, the N--formyl-dimethylamino, hydrogen, tertiary butyl formyl radical, the cyclopentyl ethanoyl, cyclopropane carbonyl, the cyclobutylmethyl acyl group, the cyclohexyl formyl radical, the 2-furancarbonyl, the 2-Thenoyl, 2-chloropyridine-3-formyl radical, 6-chloropyridine-3-formyl radical, to the tert.-butylbenzene formyl radical, the 2-nitro benzoyl, the 3-nitro benzoyl, 3, the 5-dinitrobenzoyl, the 2-fluoro benzoyl, the 3-fluoro benzoyl, the 2-chlorobenzene formacyl, the 3-chlorobenzene formacyl, the 4-chlorobenzene formacyl, the 2-methyl benzoyl, the 3-methyl benzoyl, the 4-methyl benzoyl, 3,5-dimethylbenzoyl, 2-trifluoromethyl benzoyl, 3-trifluoromethyl benzoyl, 4-trifluoromethyl benzoyl, the 2-anisoyl, the 3-anisoyl, the 4-anisoyl, 4-cyano group benzoyl, ethoxycarbonylmethyl group; N=0,1,2.

2. the described 4-methyl isophthalic acid of claim 1, the synthetic method of 2,3-thiadiazoles-5-triazole class compounds I, concrete synthetic route is as follows:

Wherein: RCO is selected from: N, the N-formyl-dimethylamino, hydrogen, tertiary butyl formyl radical, the cyclopentyl ethanoyl, cyclopropane carbonyl, the cyclobutylmethyl acyl group, the cyclohexyl formyl radical, the 2-furancarbonyl, the 2-Thenoyl, 2-chloropyridine-3-formyl radical, 6-chloropyridine-3-formyl radical, to the tert.-butylbenzene formyl radical, the 2-nitro benzoyl, the 3-nitro benzoyl, 3, the 5-dinitrobenzoyl, the 2-fluoro benzoyl, the 3-fluoro benzoyl, the 2-chlorobenzene formacyl, the 3-chlorobenzene formacyl, the 4-chlorobenzene formacyl, the 2-methyl benzoyl, the 3-methyl benzoyl, the 4-methyl benzoyl, 3,5-dimethylbenzoyl, 2-trifluoromethyl benzoyl, 3-trifluoromethyl benzoyl, 4-trifluoromethyl benzoyl, the 2-anisoyl, the 3-anisoyl, the 4-anisoyl, 4-cyano group benzoyl, ethoxycarbonylmethyl group; N=0,1,2;

Specifically be divided into following steps:

Compound I I15.8 is restrained, i.e. 0.1 mole and potassium sulfocyanate 19.4 grams, namely 0.2 mole, add in 25 milliliters the flask, add 10 milliliters of hydrochloric acid solns: hydrochloric acid soln is made up of 2 milliliter of 37% concentrated hydrochloric acid and 8 ml waters, stirs it is mixed, reacted 4-5 hour down in 80-90 degree centigrade, the adularescent solid is separated out in the reaction process, and after the ice bath cooling, suction filtration gets solid chemical compound III, obtain 11.9 grams after the oven dry, productive rate is 55%; The amount of intermediate III preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle;

With compound III 2.17 grams, i.e. 10 mmoles, add in 100 milliliters the flask with the 5%NaOH40 milliliter, stirring mixes it, and back flow reaction 4-5 hour, then with its ice bath cooling, the hydrochloric acid soln that adds 2 mol is regulated pH=5, have flaxen solid to separate out, suction filtration also uses the saturated common salt water washing to get compound IV 1.8 grams after the drying again, and productive rate is 85%;

The amount of intermediate compound IV preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle;

With compound IV 0.39 gram, i.e. 2.0 mmoles, with salt of wormwood 0.41 gram, i.e. 3.0 mmoles, add in 25 milliliters the flask, add ethyl chloroacetate 0.24 gram simultaneously, namely 2.0 mmoles add 6.5 milliliters of dehydrated alcohols, stirring mixes it, oil bath back flow reaction 2 hours is removed ethanol with its decompression then, and the hydrochloric acid soln that adds 2 mol is regulated pH=5, again it is got organic layer with dichloromethane extraction, organic layer is used saturated sodium bicarbonate solution in succession, each washing of saturated nacl aqueous solution is once used anhydrous sodium sulfate drying then, and suction filtration is removed anhydrous sodium sulphate, the concentrating under reduced pressure desolventizing, get compound V0.38 gram through 200～300 order purification by silica gel column chromatography, eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, productive rate are 67%; The amount of compound V preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle;

At ice bath with under stirring, with compound V0.49 gram, namely 1.75 mmoles with 10 milliliters of methylene dichloride dissolvings, add MCPBA then in batches; When n=1, the MCPBA consumption is 1.75 mmoles; When n=2, the MCPBA consumption is 4.38 mmoles; Reaction mixture reaction 3 hours, the adularescent solid occurs in the reaction process; Concentrating under reduced pressure reaction solution behind the stopped reaction gets compound VI or VII through 200～300 order purification by silica gel column chromatography, and eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, and its productive rate is respectively 52.1% and 44.2%; The amount of compound VI or VII preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle;

Get in the flask that compound V2.0 mmole and triethylamine 4.0 mmoles join 25 milliliters, add the DMAP0.2 mmole, add 10 milliliters of 10 milliliters of anhydrous methylene chlorides or tetrahydrofuran (THF)s, stirring mixes it, drip 5 milliliters of the dichloromethane solution contain the RCOCl1.5 mmole or tetrahydrofuran (THF)s with addition funnel under the ice bath, dropwise under the normal temperature of back and reacted 4-5 hour, then reaction solution is diluted with 30 milliliters of methylene dichloride, use 2 mol HCl respectively, saturated sodium bicarbonate solution, each washing of saturated nacl aqueous solution once, use the anhydrous sodium sulfate drying organic layer then, concentrate, with 200-300 order silica gel column chromatography separating purification product VII I, eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, with the pure product calculated yield of gained; Its physical and chemical parameter and structural parameter see Table 1;

At ice bath with under stirring, with compound VIII 1.75 mmoles, with 10 milliliters of methylene dichloride dissolvings, add MCPBA then in batches; When n=1, the MCPBA consumption is 1.75 mmoles; When n=2, the MCPBA consumption is 4.38 mmoles; Reaction mixture reaction 3 hours, the adularescent solid occurs in the reaction process; Concentrating under reduced pressure reaction solution behind the stopped reaction gets compound I X or X through 200～300 order purification by silica gel column chromatography, and eluent is that volume ratio is 3: 1 to 10: 1 60-90 degree centigrade sherwood oil: ethyl acetate, calculate productive rate with its pure product of gained; The amount of compound I X or X preparation and the volume of reaction vessel enlarge by corresponding proportion or dwindle.

3. the described 4-methyl isophthalic acid of claim 1,2,3-thiadiazoles-5-triazole class compounds I goes up the purposes of acceptable assistant in the preparation sterilant with agricultural.

4. the described 4-methyl isophthalic acid of claim 1,2,3-thiadiazoles-5-triazole class compounds I goes up the purposes of acceptable assistant in the preparation sterilant with agricultural.

5. the described 4-methyl isophthalic acid of claim 1,2,3-thiadiazoles-5-triazole class compounds I goes up the purposes of acceptable assistant in the preparation anti-plant virus agent with agricultural.

6. the described 4-methyl isophthalic acid of claim 1, the application in 2,3-thiadiazoles-5-triazole class compounds I and sterilant combination control agricultural and forestry and the gardening plant insect pest:

All 4-methyl isophthalic acids of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and existing sterilant: Chlorpyrifos 94, the inferior Nong in ground, acetamiprid, Affirm (Merck Co.), more visit rhzomorph, Avrmectin, pleocidin, fenvalerate, efficient fenvalerate, Cypermethrin, effective cypermethrin, lambda-cyhalothrin, Deltamethrin, Fenvalerate, the Beta-cyfloxylate, cyfloxylate, the Lambda-lambda-cyhalothrin, Permanone, permethrin, esbiothrin, cyhalothrin, bifenthrin, permethrin, ether chrysanthemum ester, flumethrin, fluvalinate, Provado, acetamiprid, Ti304, imidaclothiz, thiophene worm quinoline, thiophene worm piperazine, thiophene worm amine, MTI-446, clothianadin, Da Tenan, diflubenzuron, young urea goes out, Teflubenzuron, deinsectization is grand, fluorine bell urea, flufenoxuron, the pyridine worm is grand, the Acarus tritici urea, the poisonous insect urea, penfluron, Noviflumuron is noviflumuron, and its CAS number is 121451-02-3, flucycloxuron, Novaluron is Rimon, fluorine pyridine urea, Bay sir6874 i.e. { 1-[(3.5-two chloro-4) 4-nitrophenoxy phenyl 3-3-(2-chlorobenzene)-urea }, Bay SIR-8514 i.e. [1-(4-Trifluoromethoxyphen-l)-3-(2-chlorobenzene)-urea], piperazine worm urea, namely two three flufenoxuron of Bistrifluron, furans worm hydrazides, the worm hydrazides, chlorine worm hydrazides, methoxyfenozide, ring worm hydrazides, Rogor, omethoate, SD-1750, acephate, triazophos, Resitox, pyridaphenthione, isazofos, Ro 7-5050, SevinCarbaryl, Aphox, meta-tolyl-N-methylcarbamate (MTMC), isoprocarb, cartap, fenobucarb, leaf disperses, carbaryl, benfuracarb, carbosulfan, cartap, bromopropylate, hexythiazox, azoles mite ester, pyridaben, four mite piperazines, alkynes mite spy, the butyl ether urea, benfuracarb, pyrrole aphid ketone, spiral shell mite ester, spiral shell worm ester, spiral shell worm ethyl ester, butene-fipronil, azocyclotin, Buprofezin, ethoprophos, fluorine worm nitrile, the desinsection list, disosultap, the chlorine insect amide, Flubendiamide, the fluorine cyanogen insect amide, cyanogen insect amide, Tolfenpyrad, tebufenpyrad, bromothalonil, pyrazine ketone, second mite azoles, tebufenpyrad, the young ketone of rattling away, the pyrrole propyl ether, in the emaricin etc. any one or two kinds are used in combination for control agricultural and forestry and gardening plant insect pest; 4-methyl isophthalic acid of the present invention, 2, the 3-thiadiazoles-quality percentage composition of 5-triazole class compounds I in composition is 1%-90%, 4-methyl isophthalic acid of the present invention, the ratio of 2,3-thiadiazoles-5-triazole class compounds I and above-mentioned sterilant is mass percent 1%: 99% to 99%: 1%; Spray after can directly converting water, comprise agricultural in the preparation of composition and go up acceptable solvent and emulsifying agent and solubility promoter and synergistic agent etc., the formulation of composition processing is selected from sustained release dosage, pulvis, micro-capsule suspension, the dispersible body preparation, the dispersible solid preparation, seed treatment emulsion, aqueous emulsion, granule, microemulsion, finish, seed with coated pesticidal, suspended emulsion agent, soluble thick agent, poison grain, aerosol, block poison bait, sustained-release block, dense poison bait, capsule suspension, can disperse dense dose, missible oil, the electrostatic spray agent, water-in-oil emulsion, seed treatment agent, oil-in-water emulsion, smoke candle, granula subtilis, smoke candle, smoke cartridge, the smog rod, the smog sheet, smoke substance, the smog ball, granular poison bait, foaming agent, ointment, thermal fog, solid-liquid mixes the dress agent, liquid/liquid mixes the dress agent, cold mist agent, Gu Gu/mix and adorn agent, the medicine lacquer, the seed treatment liquor, microgranules, oil suspending agent, finish, the oil-dispersing property pulvis, paste, the sheet poison bait, dense jelly, sprinkle and water agent, stylus, plant the clothing agent, poison bait, basting agent, the fritter poison bait, suspension agent, suspension emulsion, water-soluble granule, soluble thick agent, the film forming finish, tablet, follow the trail of pulvis, ultra low volume liquids, in the steam releasing agent any one; The insect pest that can prevent and treat mainly contains red spider, Asiatic migrotory locust, clouding car locust, Chinese rice grasshopper, Patanga japonica (l.Bol.), single thorn mole cricket, the east mole cricket, rice thrips, onion thrips, greenhouse thrips, haplothrips aculeatus, Mai Jian manages thrips, Trialeurodes vaporariorum Westwood, Bemisia tabaci, rice green leafhopper, green leaf hopper, chlorita biguttula, spot clothing plant hopper, brown paddy plant hopper, white backed planthopper, small brown rice planthopper, the flat angle of sugarcane plant hopper, cotten aphid, green bugs, grain aphid, black peach aphid, kaoliang aphid, radish aphid, icerya purchasi, Pseudaulacaspis pentagona, unaspis shield kuwana, san jose scale, wax insect, ceroplastes rubens, the hard a red-spotted lizard of Korea's ball, pear lace bug, the banana lace bug, thin corner piece stinkbug, little minute pirate bugs, slender rice bug, paddy fly, niphe elongata, scotinophora lurida, Nezara viridula smaragdula Fabricius., green plant bug, alfalfa plant bug, black striped plant bug, chrysopa septempunctata, beautiful Chrysopa, Chinese green lacewing, rain moth, casemaking clothes moth, cnidocampa flavescens walker, brown slug moth, thosea siensis, gelechiid, pink bollworm, brachmia triannuella, small cabbage moth, small heart-eating peach worm, eating-core bean worm, small heart-eating peach worm, the apple Spilonota lechriaspis, brown belt length leaf roller, intend smaller apple leaf roller, striped rice borer, bean-pod borer, Pyrausta nubilalis (Hubern)., yellow rice borer, Oeobia undalis, Cnaphalocrocis medinali(rice leaf roller), the bar snout moth's larva, the wild snout moth's larva of lap leaf, dichocrocis punctiferalis, armyworm, prodenia litura, rice green caterpillar, anomis flava, beet armyworm, pink rice borer, bollworm, ancient cooking vessel point diamond drill, black cutworm, big cutworm, yellow cutworm, steal poison moth, gypsymoth, palaearctic sweet potato, greenish brown hawk moth, the straight burr rice hesperiidae, pelopidas mathias, the oranges and tangerines swallowtail butterfly, Common Mormon, small white, pyrameis indica, the yellow a kind of butterfly harmful to crop plants of ramie, the beans blister beetle, the Venus ground beetle, wrinkle sheath ground beetle, wheat head ground beetle, pleonomus canaliculatus, Agriotes subrittatus Motschulsky, khapra beetle, attagenus piceus, the little buprestid beetle of oranges and tangerines, gold edge buprestid beetle, tenebrio molitor, dark mealworm, red flour beetle, confused flour beetle, the verdigris different beetle, black dull cockchafer, holotrichia oblita, mulberry borer, longicorn beetle, nadezhdiella cantori, pink neck longicorn, big daikon leaf beetle, daicon leaf beetle, aulacophora femoralis, Phyllotreta striolata, Callosobruchus chinensis, pea weevil, broad bean weevil, sitophilus zea-mais, rice weevil, dolerus tritici, pear fruit sawfly, the yellowish leukorrhea ichneumon wasp, armyworm white star ichneumon wasp, corn earworm is hanged the cocoon ichneumon wasp, bollworm tooth lip ichneumon wasp, snout moth's larva stain wart ichneumon wasp, mosquito, fly, horsefly, wheat midge, contarinia tritici, pachydiplosis oryzae, citrus fruit fly, the melon trypetid, the latent fly of wheat leaf ash, Americal rice leaf miner, the black fly of diving of beans stalk, frit fly, plant fly, onion fly, the radish fly, full skirt chases after posts fly, Pyrausta nubilalis (Hubern). is strict posts fly, armyworm lacks Agricultural pests such as must posting fly, forestry pest; Plant in control agricultural and forestry and the gardening plant insect pest comprises paddy, wheat, barley, oat, corn, Chinese sorghum, sweet potato, potato, cassava, soybean, pea-pods, broad bean, pea, mung bean, red bean, cotton, silkworm and mulberry, peanut, rape, sesame, Sunflower Receptacle, beet, sugarcane, coffee, cocoa, genseng, the bulb of fritillary, rubber, coconut, oil palm, sisal hemp, tobacco, tomato, capsicum, radish, cucumber, Chinese cabbage, celery, hot pickled mustard tube, beet, rape, green onion, garlic, watermelon, muskmelon, hami melon, pawpaw, really, tea, wild vegetable, bamboo shoots, hops, paddy rice, pepper, apple, banana, citrus, peach, papaya, orchid, potted landscape; Composition has improved the defence capability of plant in desinsection, make plant produce defence capability to pathogenic fungi, bacterium and virus infection.

7. the described 4-methyl isophthalic acid of claim 1, the application during 2,3-thiadiazoles-5-triazole class compounds VII and miticide combination control agricultural and forestry and gardening plant mite do harm to:

8. the described 4-methyl isophthalic acid of claim 1, the application in 2,3-thiadiazoles-5-triazole class compounds VII and sterilant combination control agricultural and forestry and the gardening plant disease:

all 4-methyl isophthalic acids of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and existing bactericide such as diazosulfide, tiadinil, be abbreviated as TDL, tisocromide, the first thiophene lures amine, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-formic acid, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-sodium formate, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-Ethyl formate, the DL-beta-aminobutyric acid, isotianil, it is English general by name: isotianil, 3,4-, two chloroisothiazoles-5-formic acid, 3,4-, two chloroisothiazoles-5-sodium formate, 3,4-, two chloroisothiazoles-5-Ethyl formate, virazole, antofine, Ningnanmycin or salicylic acid, frost urea cyanogen, thiram, ziram, Mancozeb, aliette, thiophanate-methyl, Bravo, the enemy can be loose, procymidone, fenpropidin, thiophanate methyl, thiophanate, Metalaxyl-M, flumorph, dimethomorph, efficient metalaxyl, efficient M 9834, two chlorine zarilamids, flusulfamide, the first flusulfamide, thiophene fluorine bacterium amine, flutolanil, tecloftalam, ring propionyl bacterium amine, cyflufenamid, fenhexamid, zarilamid, Silthiopham, furametpyr, the pyrrole metsulfovax, mandipropamid, zoxamide, fenfuram, carboxin, chlozolinate, iprodione, Fluoxastrobin, dimoxystrobin, fluoxastrobin, kresoxim-methyl, SSF 126, orysastrobin, ZEN 90160, pyraclostrobin, oxime bacterium ester, Enestroburin, alkene oxime amine, oxygen ring azoles, bromuconazole, Cyproconazole, Difenoconazole, alkene azoles alcohol, efficient alkene azoles alcohol, epoxiconazole, RH-7592, Fluquinconazole, Flusilazole, Flutriafol, own azoles alcohol, glyoxalin, plant the bacterium azoles, metconazole, nitrile bacterium azoles, penconazole, propiconazole, prothioconazoles, simeconazoles, Tebuconazole, tetraconazole, Triadimenol, triticonazole, bitertanol, probenazole, furidazol, imazalil, efficient imazalil, Prochloraz, fluorine bacterium azoles, cyazofamid, Fenamidone, the Evil imidazoles, pefurazoate, famoxadone, SYP-Z048, hymexazo, the spirit of Evil frost, Guardian, Grandox fumigant, octhilinone, benthiozole, dodemorph, butadiene morpholine, tridemorph, fenpiclonil, fludioxonil, fluazinam, pyrifenox, ring pyridine bacterium amine, Boscalid, fluopicolide, pyridine bacterium amine, cyprodinil, the fluorine mepanipyrim, ferimzone, mepanipyrim, phonetic mould amine, Fenarimol, nuarimol, chinomethionat, dithianon, ethoxyquin, oxyquinoline, the third oxygen quinoline, benzene oxygen quinoline, the mould prestige of second, iprovalicarb, the benzene metsulfovax, Propamocarb, methasulfocarb, edifenphos, IBP, pyrazophos, tolelofos-methyl, blasticidin-S, kasugarnycin, polyoxin, Polyoxin, valida, jinggangmeisu, streptomysin, metalaxyl, furalaxyl, M 9834, ofurace, mebenil, carbendazim, benomyl, thiophanate-methyl, triazolone, bupirimate, dimethirimol, the phonetic phenol of second, difoltan, captan, folpet, vinclozolin, fluoromide, dimethachlon, Bravo, Isoprothiolane, kitazine, Yekuzuo, pentachloronitrobenzene, Propineb, phosethyl-Al, sulphur, Bordeaux mixture, copper sulphate, copper oxychloride, cuprous oxide, Kocide SD, metrafenone, Pencycuron, diclomezin, Rabcide, pyroquilon, volution bacterium amine, tricyclazole, triforine, the pyridine of many fruits, the hot salt of biguanides, iminoctadine, botran, the benzene flusulfamide, the toluene flusulfamide, K-281, fenaminosulf, oxolinic acide, probenazole, bronopol, iodomethane, metham-sodium, enemy's line ester, dazomet, nemamort, lythidathion, cadusafos, fensulfothion, thionazin, fenamiphos, phonamiphos, dichlofenthion, isazofos, fosthietan, oxamyl, Aldicarb, carbofuran, vikane, dichloropropylene, dichloro-isonicotinic acid, other known any any one or two kinds that can be used as in bactericide such as allyl isothiazole are used in combination for control agricultural and forestry and gardening plant disease, 4-methyl isophthalic acid of the present invention, the total quality percentage composition of 2,3-thiadiazoles-5-triazole class compounds I in composition is 1%-90%, 4-methyl isophthalic acid of the present invention, the ratio of 2,3-thiadiazoles-5-triazole class compounds I and aforementioned bactericide is mass percent 1%: 99% to 99%: 1%, the prevention effect of composition is good, and these compositions have certain synergistic effect and summation action, does not find to have the composition of antagonistic action, above-mentioned composition can be used for the control of agricultural plant disease and gardening plant disease, controlling object comprises that more than 20 of the Achylas, Aphanomyces, pythium, Phytophthora, Sclerospora, Plasmopara, Pseudoperonospora, Peronospora of Oomycete etc. belong to the diseases that produce, as other diseases of plurality of cereals crop, industrial crops, gardening plant and the forestry plants such as seedling blight of rice, tomato root maize ear rot, the late blight of potato, black shank, millet powdery mildew, downy mildew of garpe, downy mildew of lettuce, cucumber downy mildew, cucumber anthracnose etc., the formulation of composition processing is selected from sustained release agent, pulvis, micro-capsule suspension, the dispersible body preparation, the dispersible solid preparation, seed treatment emulsion, aqueous emulsion, granule, microemulsion, finish, seed with coated pesticidal, suspension emulsion, soluble thick agent, poison grain, aerosol, block poison bait, sustained-release block, dense poison bait, capsule suspension, can disperse dense dose, missible oil, the electrostatic spray agent, water-in-oil emulsion, seed treatment, oil in water emulsion, smoke candle, granula subtilis, smoke candle, smoke cartridge, the smog rod, the smog sheet, smoke agent, the smog ball, granular poison bait, foaming agent, ointment, thermal fog, solid-liquid mixes the dress agent, liquid/liquid mixes the dress agent, cold mist agent, Gu Gu/mix filling agent, the medicine paint, the seed treatment liquor, fine granule, oil suspending agent, finish, the oil-dispersing property pulvis, paste, the sheet poison bait, dense jelly, sprinkle and water agent, stylus, seed coat agent, poison bait, liniment, the fritter poison bait, suspending agent, suspended emulsion, water-soluble granule, soluble thick agent, the film forming finish, tablet, follow the trail of pulvis, ultra low volume liquids, any one in the steam releasing agent, these compositions are used for control agricultural and forestry and the applicable plant of gardening plant disease and comprise cereal: paddy, wheat, barley, oat, corn, millet, Chinese sorghum, tuber crops: sweet potato, potato, cassava, beans: soybean, broad bean, pea, mung bean, red bean and fiber: cotton, crudefiber crop, silkworm and mulberry, oil plant: peanut, rape, sesame, soybean, sunflower, sugar material: beet, sugarcane, beverage: tealeaves, coffee, cocoa, hobby: tobacco leaf, medicinal: ginseng, the bulb of fritillary, the torrid zone: rubber, coconut, oil palm, sisal hemp, cereal crops and fruit, flowers, oil plant, sugar material and cotton, fiber crops, tea, tobacco, Chinese medicine industrial crops and plant melon, really, tea, silkworm and mulberry, vegetables, contain various wild vegetables, bamboo shoots, flowers and ornamental plant, hops, medicinal material, pepper, seedling and other garden crops such as tobacco: flue-cured tobacco, air-curing of tobacco leaves, suncured tabacco, vegetables, tomato, capsicum, radish, cucumber, Chinese cabbage, celery, hot pickled mustard tube, beet, rape, green onion, garlic, melon: watermelon, muskmelon, "Hami" melon, pawpaw, beans: soybean, broad bean, garden pea, potato, wheat, corn, paddy rice, peanut, fruit tree: apple, banana, citrus, peach, papaya, flowers: orchid, potted landscape, composition has improved the defence capability of plant in sterilization, make plant produce defence capability to disease fungus, bacterium and virus infection.

9. the described 4-methyl isophthalic acid of claim 1, the application in 2,3-thiadiazoles-5-triazole class compounds VII and anti-plant virus agent combination control agricultural and forestry and the gardening plant virus disease:

4-methyl isophthalic acid of the present invention, 2,3-thiadiazoles-5-triazole class compounds I and existing Antiphytoviral medicament diazosulfide, tiadinil, be abbreviated as TDL, different metsulfovax, it is English general by name: isotianil, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-formic acid, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-sodium formiate, the 4-methyl isophthalic acid, 2,3-thiadiazoles-5-ethyl formate, 3,4-two chloroisothiazoles-5-formic acid, 3,4-, two chloroisothiazoles-5-sodium formiate, 3,4-, two chloroisothiazoles-5-ethyl formate, the DL-beta-aminobutyric acid, virazole, antofine, Ningnanmycin, tisocromide, the first thiophene lures amine or Whitfield's ointment, cytosintetidemycin, dichloro-isonicotinic acid, allyl isothiazole, well ridge azanol, any 1 or the combination of 2 compounds are used for control agricultural and forestry and gardening plant virus disease in the jingganmycin; The disease of control agricultural and forestry and gardening plant virus disease is selected from tobacco mosaic virus disease, various melon virus diseases, various solanberry viroid diseases, the beans virus disease, the Cruciferae virus disease, the grain and oil crop virus disease, any in cotton virus disease and the various fruit tree virus disease, wherein endanger serious being selected from: tobacco virus, peppery pimento virus disease, tomato virus disease, Chinese cabbage virus disease, the paddy rice virus disease comprises rice dwarf virus disease, yellow dwart, stripe virus disease, the fern leaf of tomato viral disease, sick and the tobacco veinal necrosis virus disease of chilli pepper mosaic virus, the corn short mosaic disease, cauliflower mosaic virus, the oranges and tangerines virus disease, cymbidium mosaic virus, any in the cybidium ring spot virus; The plant that these compositions are used for control agricultural and forestry and gardening plant virus disease is selected from paddy, wheat, barley, oat, corn, Chinese sorghum, sweet potato, potato, cassava, soybean, pea-pods, broad bean, pea, mung bean, red bean, cotton, silkworm and mulberry, peanut, rape, sesame, Sunflower Receptacle, beet, sugarcane, coffee, cocoa, genseng, the bulb of fritillary, rubber, coconut, oil palm, sisal hemp, tobacco, tomato, capsicum, radish, cucumber, Chinese cabbage, celery, hot pickled mustard tube, beet, rape, green onion, garlic, watermelon, muskmelon, hami melon, pawpaw, really, tea, wild vegetable, bamboo shoots, hops, potato, paddy rice, pepper, apple, banana, citrus, peach, papaya, orchid, agriculturals such as potted landscape, gardening, economical, plants such as forestry; The use of these compositions makes the immunizing power of crop self improve, and has induced the defence capability of plant generation to viral diseases of plants when producing the control of insect especially infection insect; Also can produce the direct prevention effect of virus disease; Therefore, these compositions can be used for Antiphytoviral medicament and inducing plant Antiphytoviral medicaments preparation and purposes; 4-methyl isophthalic acid of the present invention, 2, the total quality percentage composition of 3-thiadiazoles-5-triazole class compounds I in composition is 1%-90%, 4-methyl isophthalic acid of the present invention, the ratio of 2,3-thiadiazoles-5-triazole class compounds I and aforementioned Antiphytoviral medicament is mass percent 1%: 99% to 99%: 1%; The formulation of composition processing is selected from sustained release dosage, pulvis, micro-capsule suspension, the dispersible body preparation, the dispersible solid preparation, seed treatment emulsion, aqueous emulsion, granule, microemulsion, finish, seed with coated pesticidal, suspended emulsion agent, soluble thick agent, poison grain, aerosol, block poison bait, sustained-release block, dense poison bait, capsule suspension, can disperse dense dose, missible oil, the electrostatic spray agent, water-in-oil emulsion, seed treatment agent, oil-in-water emulsion, smoke candle, granula subtilis, smoke candle, smoke cartridge, the smog rod, the smog sheet, smoke substance, the smog ball, granular poison bait, foaming agent, ointment, thermal fog, solid-liquid mixes the dress agent, liquid/liquid mixes the dress agent, cold mist agent, Gu Gu/mix and adorn agent, the medicine lacquer, the seed treatment liquor, microgranules, oil suspending agent, finish, the oil-dispersing property pulvis, paste, the sheet poison bait, dense jelly, sprinkle and water agent, stylus, plant the clothing agent, poison bait, basting agent, the fritter poison bait, suspension agent, suspension emulsion, water-soluble granule, soluble thick agent, the film forming finish, tablet, follow the trail of pulvis, ultra low volume liquids, in the steam releasing agent any one; All show addition or synergism between these compositions, when keeping insecticidal activity, the effect that its antiviral activity all uses separately greater than any one compound; Find no the composition of antagonistic action, the drug effect lasting period of composition is long.

10. the described 4-methyl isophthalic acid of claim 1,2,3-thiadiazoles-5-triazole class compounds VII and common pesticide combination form the complete processing of pesticide preparation.