Liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine, their preparation methods and applications

Abstract

This invention relates to liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine, their preparation methods, and applications, belonging to the field of agricultural chemicals technology. The liquid formulations of this invention, containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine, by compounding 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine with different compounding agents and selecting specific cosolvents, can achieve good sustained foaming properties, dilution stability, low-temperature stability, and thermal storage stability. The liquid formulations of this invention, containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine, inhibit the decomposition of chlorophyll, nucleic acids, and proteins in plants, thus playing a role in preserving green color and preventing aging; they also have multiple functions such as regulating amino acids, auxins, and inorganic salts, and can be widely used in all stages of agriculture, fruit trees, and horticultural crops from germination to harvest.

Description

TECHNICAL FIELD

[0001] The present application relates to a liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine and its preparation method and application, belonging to the technical field of agrochemicals. BACKGROUND

[0002] According to the China Pesticide Industry Association, 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine (Anisiflupurin) is a new fluorine-containing purine cell division element announced by ISO, its chemical abstracts service registration number is 1089014-47-0; the international generic name is anisiflupurin (P); the Chinese chemical name is 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine; the molecular formula is C 12 H 10 FN5O; the relative molecular mass is 259.239; the melting point is 195℃; it is a 6-anilino purine derivative; its chemical structure is as follows:

[0003]

[0004] Anisiflupurin technical material is white crystalline powder, slightly soluble in water, slightly soluble in ethanol, stable in acid and alkali. Anisiflupurin is a 6-anilino purine derivative; in agriculture, it can stimulate the growth of tobacco callus, maintain the chlorophyll content in isolated wheat leaves, and induce the synthesis of β-carotene in amaranth cotyledons, and has an inhibitory effect on cell division element oxidation / dehydrogenase induced by abiotic stress. And in vitro test results show that anisiflupurin has low toxicity, and the toxicity of mammalian osteosarcoma cell line HOS, breast cancer cell line MCF-7 and mouse cell line fibroblast NIH-3T3 is comparable to that of kinetin. After 80 passages, it is better than kinetin in anti-aging of human fibroblasts. Therefore, Anisiflupurin has the advantages of low toxicity and good safety in use.

[0005] At present, many plant growth regulators alone often cannot achieve the desired effect, and the main disadvantages of single agent application are that the biological activity is relatively single, the growth regulation effect is relatively low, the use concentration is large, and the growth regulation effect can usually be played only in a certain growth period of crops. Therefore, it is necessary to correctly and reasonably select and mix different plant growth regulators to overcome or avoid side effects, so as to achieve the expected application effect, that is, to achieve synergistic, additive or induction effect, and to avoid antagonistic effect. However, at present, there is no report and registration on the preparation prepared by compounding Anisiflupurin with other compounds.

[0006] Therefore, it is urgent to develop a liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine with good stability, so as to better improve the biological activity and growth regulation effect of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine. SUMMARY

[0007] The present application aims to provide a liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine, which can solve the problem of single activity and poor plant growth regulation effect when 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine is used alone.

[0008] The second object of the present application is to provide a preparation method of a liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine, which can solve the problem of single activity and poor plant growth regulation effect when 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine is used alone as a liquid formulation.

[0009] The third object of the present application is to provide the application of a liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine as a plant growth regulator, which can solve the problem of single activity and poor plant growth regulation effect when 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine is used alone as a plant growth regulator.

[0010] In order to achieve the above objects, the technical scheme adopted by the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present application is as follows:

[0011] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine is mainly composed of active ingredients, emulsifiers, solvents and cosolvents; the active ingredients are composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and a complex; the complex is gibberellic acid GA3, gibberellic acid GA4+7, 24-epibrassinolid, 28-homobrassinolid, amino acid ester, ethylene or triacontanol; the cosolvent is dimethyl sulfoxide, N,N-dimethylformamide, N-methyl pyrrolidone, lactic acid; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid formulation is not more than 10%; the mass fraction of the complex in the liquid formulation is not more than 30%.

[0012] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of the present application, by compounding 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine with different compounds, and selecting specific cosolvents, can make the liquid preparation have good long-lasting foaming property, dilution stability, low-temperature stability and heat storage stability. The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of the present application has the effect of transporting amino acids, auxins, inorganic salts and the like to the growth sites, and can be widely used in various stages from germination to harvesting of agricultural, fruit tree and horticultural crops.

[0013] Preferably, the compound is gibberellic acid GA3, gibberellic acid GA4+7, 24-epibrassinolide, 28-homobrassinolide, amaranth or triacontanol, and the liquid preparation further comprises a stabilizer, which is formic acid, acetic acid, lactic acid, 2,6-di-tert-butyl-p-cresol or tert-butyl hydroquinone. The stabilizer ensures that the preparation remains uniform in the dilution liquid without precipitates during dilution with water, and facilitates use by farmers and avoids clogging of the atomizing nozzles of pesticide equipment.

[0014] Preferably, the compound is gibberellic acid GA3, and the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine and gibberellic acid GA3 in the liquid preparation is independently not more than 0.9%;

[0015] or the compound is gibberellic acid GA4+7, and the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine and gibberellic acid GA4+7 in the liquid preparation is independently not more than 1.8%;

[0016] or the compound is 24-epibrassinolide, and the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the liquid preparation is not more than 1.99%, and the mass fraction of 24-epibrassinolide is not more than 0.01%;

[0017] or the compound is 28-homobrassinolide, and the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the liquid preparation is not more than 4.995%, and the mass fraction of 28-homobrassinolide is not more than 0.005%;

[0018] or the compound is amaranth, and the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the liquid preparation is not more than 2%, and the mass fraction of amaranth is not more than 8%;

[0019] Or the complex is ethephon, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is not more than 0.5%, and the mass fraction of ethephon is not more than 29.5%;

[0020] Or the complex is triacontanol, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is not more than 9.8%, and the mass fraction of triacontanol is not more than 0.2%. In different liquid preparations, the content of the active ingredient is too high, which can cause precipitation, crystallization, delamination and other phenomena during normal temperature storage.

[0021] Preferably, the complex is gibberellic acid GA3, and the stabilizer is formic acid and / or lactic acid; the mass fraction of the stabilizer in the liquid preparation is 0.5-2%;

[0022] Or the complex is gibberellic acid GA4+7, and the stabilizer is formic acid and / or lactic acid; the mass fraction of the stabilizer in the liquid preparation is 10-20%;

[0023] Or the complex is 24-epibrassinolid, and the stabilizer is formic acid and / or acetic acid; the mass fraction of the stabilizer in the liquid preparation is 3-6%;

[0024] Or the complex is 28-homobrassinolid, and the stabilizer is formic acid and / or acetic acid; the mass fraction of the stabilizer in the liquid preparation is 0.3-0.6%;

[0025] Or the complex is amaranth, and the stabilizer is 2,6-di-tert-butyl-p-cresol or tert-butyl-hydroquinone; the mass fraction of the stabilizer in the liquid preparation is 1-3%;

[0026] Or the complex is triacontanol, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is not more than 1.9%, the mass fraction of triacontanol in the liquid preparation is not more than 0.1%, and the stabilizer in the liquid preparation is acetic acid; the mass fraction of the stabilizer in the liquid preparation is 1-3%;

[0027] Or the complex is 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is > 1.9% and ≤ 9.8%, the mass fraction of triacontanol in the liquid preparation is > 0.1% and ≤ 0.2%, and the stabilizer in the liquid preparation is formic acid; the mass fraction of the stabilizer in the liquid preparation is 6-10%. The type and amount of the stabilizer have an important influence on the physical stability of the liquid preparation, and for different complexes, the corresponding stabilizer and the corresponding amount of the stabilizer need to be used. If the type and amount of the stabilizer are changed, the performance of the liquid preparation will not meet the standard. When the amount of the stabilizer is too much, the pH value of the preparation will be too low, which will cause the decomposition of the active ingredient. When the amount of the stabilizer is too little, the water dilution of the preparation will have a precipitate, and the dilution stability will not meet the standard.

[0028] Preferably, the complex is gibberellic acid GA3, the emulsifier in the liquid preparation is octylphenol polyoxyethylene ether and / or fatty alcohol polyoxyethylene ether; the mass fraction of the emulsifier in the liquid preparation is 1-4%;

[0029] Or the complex is gibberellic acid GA4+7, the emulsifier in the liquid preparation is octylphenol polyoxyethylene ether and / or fatty alcohol polyoxyethylene ether; the mass fraction of the emulsifier in the liquid preparation is 2-4%;

[0030] Or the complex is 24-epibrassinolide, the emulsifier in the liquid preparation is Tween 80; the mass fraction of the emulsifier in the liquid preparation is 3-7%;

[0031] Or the complex is 28-homobrassinolide, the emulsifier in the liquid preparation is polyethylene glycol 400; the mass fraction of the emulsifier in the liquid preparation is 4-8%;

[0032] Or the complex is amaranth, the emulsifier in the liquid preparation is polyether; the mass fraction of the emulsifier in the liquid preparation is 0.5-2%;

[0033] Or the complex is ethephon, the emulsifier in the liquid preparation is polyethylene glycol 400; the mass fraction of the emulsifier in the liquid preparation is 3-6%;

[0034] Or the complex is triacontanol, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is not more than 1.9%, the emulsifier in the liquid preparation is fatty alcohol polyoxyethylene ether; the mass fraction of the emulsifier in the liquid preparation is 2-6%;

[0035] Alternatively, the compound may be triacontanol, and the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the liquid formulation may be >1.9% and ≤9.8%, the mass fraction of triacontanol in the liquid formulation may be >0.1% and ≤0.2%, and the emulsifier in the liquid formulation may be Tween 80; the mass fraction of the emulsifier in the liquid formulation may be 3-7%. The function of the emulsifier is to reduce the interfacial tension of the components in the mixture and to form a relatively strong film on the surface of the droplets or to form an electric double layer on the surface of the droplets through the charge provided by the emulsifier, preventing the droplets from agglomerating and thus maintaining a uniform state. For different compound formulations, corresponding emulsifiers and corresponding amounts of emulsifier are required. Excessive emulsifier usage can cause: excessive viscosity of the formulation system, which is not conducive to filling and metering in actual production; turbidity of the formulation at low temperatures; and excessive dosage, leading to excessive permeability of the formulation, which can also cause phytotoxicity to crops. When the amount of emulsifier is too small, it will cause the effective ingredients of the formulation to aggregate and flocculate, resulting in the precipitation of crystals and other unqualified phenomena.

[0036] Preferably, the compound is gibberellic acid GA3, and the cosolvent in the liquid formulation is dimethyl sulfoxide; the mass fraction of the cosolvent in the liquid formulation is 15-25%.

[0037] Alternatively, the compound is gibberellic acid GA4+7, and the cosolvent in the liquid formulation is N,N-dimethylformamide; the mass fraction of the cosolvent in the liquid formulation is 30-40%.

[0038] Alternatively, the compound is 24-epibrassinolide, and the cosolvent in the liquid formulation is N-methylpyrrolidone and / or dimethyl sulfoxide; the mass fraction of the cosolvent in the liquid formulation is 10-20%.

[0039] Alternatively, the compound is 28-homobrassinolide, and the cosolvent in the liquid formulation is N-methylpyrrolidone and / or dimethyl sulfoxide; the mass fraction of the cosolvent in the liquid formulation is 20-40%.

[0040] Alternatively, the compound may be aminoethyl ester, and the cosolvent in the liquid formulation may be N-methylpyrrolidone; the mass fraction of the cosolvent in the liquid formulation may be 20-30%.

[0041] Alternatively, the compound may be ethephon, and the cosolvent in the liquid formulation may be lactic acid; the mass fraction of the cosolvent in the liquid formulation may be 30-40%.

[0042] or the complex is triacontanol, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is not more than 1.9%, the mass fraction of triacontanol in the liquid preparation is not more than 0.1%, and the cosolvent in the liquid preparation is dimethyl sulfoxide; the mass fraction of the cosolvent in the liquid preparation is 10-20%;

[0043] or the complex is triacontanol, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is >1.9% and ≤9.8%, the mass fraction of triacontanol in the liquid preparation is >0.1% and ≤0.2%, and the cosolvent in the liquid preparation is N-methyl pyrrolidone; the mass fraction of the cosolvent in the liquid preparation is 30-40%. The cosolvent dissolves the active ingredients in the liquid preparation, and can form a complex, an associated substance or a complex salt with the poorly soluble substance to increase the solubility of the drug in the solvent. The cosolvent can also increase the stability of the preparation, improve the physical properties, mask the odor and taste, reduce the irritation, improve the absorption, and increase the pharmacological effect. If the amount of the cosolvent is too small, the active ingredients in the preparation may not be completely dissolved, and unstable phenomena such as crystal precipitation may occur.

[0044] Preferably, the complex is gibberellic acid GA3, the solvent in the liquid preparation is an alcohol solvent, and the alcohol solvent is ethylene glycol and / or propylene glycol;

[0045] or the complex is gibberellic acid GA4+7, the solvent in the liquid preparation is an alcohol solvent, and the alcohol solvent is ethylene glycol and / or propylene glycol;

[0046] or the complex is 24-epibrassinolid, and the solvent in the liquid preparation is propylene glycol;

[0047] or the complex is 28-homobrassinolid, and the solvent in the liquid preparation is N,N-dimethylformamide;

[0048] or the complex is 28-homobrassinolid, and the solvent in the liquid preparation is N,N-dimethylformamide;

[0049] or the complex is 28-homobrassinolid, and the solvent in the liquid preparation is N,N-dimethylformamide;

[0050] or the complex is triacontanol, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is not more than 1.9%, the mass fraction of triacontanol in the liquid preparation is not more than 0.1%, and the cosolvent in the liquid preparation is dimethyl sulfoxide; the mass fraction of the cosolvent in the liquid preparation is 10-20%;

[0051] or the complex is triacontanol, the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is > 1.9% and ≤ 9.8%, the mass fraction of triacontanol in the liquid preparation is > 0.1% and ≤ 0.2%, and the solvent in the liquid preparation is N,N-dimethylformamide. The solvent in the liquid preparation has the following effects: ① dilution effect: the solvent can dilute the concentrated substance, making it easier to operate or handle. ② Solubilization: can dissolve substances that are not soluble in water, making them soluble substances. ③ Stabilization: the solvent can stabilize certain substances, making them less likely to be oxidized or decomposed. ④ Change the physical properties of the substance: the solvent can change the physical properties of the substance, such as viscosity, surface tension, etc., making it easier to operate or handle. If the amount of solvent is too small, the solubility of the active ingredients in the preparation will be low, incomplete dissolution will occur, and crystals will be precipitated.

[0052] Preferably, the liquid preparation is an A composition, a B composition, a C composition, a D composition, an E composition, an F composition, or a G composition.

[0053] The A composition mainly consists of active ingredients, stabilizers, emulsifiers, solvents and co-solvents; the active ingredients in the A composition consist of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and gibberellic acid GA3; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and gibberellic acid GA3 in the A composition is independently not more than 0.9%; the stabilizer in the A composition is formic acid and / or lactic acid; the mass fraction of the stabilizer in the A composition is 0.5-2%; the emulsifier in the A composition is octylphenol polyoxyethylene ether and / or fatty alcohol polyoxyethylene ether; the mass fraction of the emulsifier in the A composition is 1-4%; the solvent in the A composition is an alcohol solvent; the solvent in the A composition is ethylene glycol and / or propylene glycol; the co-solvent in the A composition is dimethyl sulfoxide; the mass fraction of the co-solvent in the A composition is 15-25%;

[0054] The B composition mainly consists of active ingredients, stabilizers, emulsifiers, solvents and co-solvents; the active ingredients in the B composition consist of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and gibberellic acid GA4+7; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and gibberellic acid GA4+7 in the B composition is independently not more than 1.8%; the stabilizer in the B composition is formic acid and / or lactic acid; the mass fraction of the stabilizer in the B composition is 10-20%; the emulsifier in the B composition is octylphenol polyoxyethylene ether and / or fatty alcohol polyoxyethylene ether; the mass fraction of the emulsifier in the B composition is 2-4%; the solvent in the B composition is an alcohol solvent; the solvent in the B composition is ethylene glycol and / or propylene glycol; the co-solvent in the B composition is N,N-dimethylformamide; the mass fraction of the co-solvent in the B composition is 30-40%;

[0055] The C composition mainly consists of active ingredients, stabilizers, emulsifiers, solvents and co-solvents; the active ingredients in the C composition consist of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and 24-epibrassinolid; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the C composition is not more than 1.99%, and the mass fraction of 24-epibrassinolid is not more than 0.01%; the stabilizer in the C composition is formic acid and / or acetic acid; the mass fraction of the stabilizer in the C composition is 3-6%; the emulsifier in the C composition is Tween 80; the mass fraction of the emulsifier in the C composition is 3-7%; the solvent in the C composition is propylene glycol; the co-solvent in the C composition is N-methyl pyrrolidone and / or dimethyl sulfoxide; the mass fraction of the co-solvent in the C composition is 10-20%;

[0056] The D composition mainly consists of active ingredients, stabilizers, emulsifiers, solvents and co-solvents; the active ingredients in the D composition consist of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and 28-homobrassinolid; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the D composition is not more than 4.995%, and the mass fraction of 28-homobrassinolid is not more than 0.005%; the stabilizer in the D composition is formic acid and / or acetic acid; the mass fraction of the stabilizer in the D composition is 0.3-0.6%; the emulsifier in the D composition is polyethylene glycol 400; the mass fraction of the emulsifier in the D composition is 4-8%; the solvent in the D composition is N,N-dimethylformamide; the co-solvent in the D composition is N-methyl pyrrolidone and / or dimethyl sulfoxide; the mass fraction of the co-solvent in the D composition is 20-40%.

[0057] The E composition is mainly composed of active ingredients, stabilizers, emulsifiers, solvents and co-solvents; the active ingredients in the E composition are composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine and malene; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the E composition is not more than 2%; the mass fraction of malene in the E composition is not more than 8%; the stabilizer in the E composition is 2,6-di-tert-butyl-p-cresol and / or tert-butyl hydroquinone; the mass fraction of the stabilizer in the E composition is 1-3%; the emulsifier in the E composition is polyether; the mass fraction of the emulsifier in the E composition is 0.5-2%; the solvent in the E composition is N,N-dimethylformamide; the co-solvent in the E composition is N-methyl pyrrolidone; the mass fraction of the co-solvent in the E composition is 20-30%; the polyether is an EO / PO block polyether;

[0058] The F composition is mainly composed of active ingredients, emulsifiers, solvents and co-solvents; the active ingredients in the F composition are composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine and ethephon; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the F composition is not more than 0.5%; the mass fraction of ethephon in the F composition is not more than 29.5%; the emulsifier in the F composition is polyethylene glycol 400; the mass fraction of the emulsifier in the F composition is 3-6%; the solvent in the F composition is selected from one or any combination of water, ethylene glycol, propylene glycol; the co-solvent in the F composition is lactic acid; the mass fraction of the co-solvent in the F composition is 30-40%;

[0059] The G composition is mainly composed of active ingredients, stabilizers, emulsifiers, solvents and co-solvents; the active ingredients in the G composition are composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine and triacontanol;

[0060] The mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the G composition is not more than 1.9%, the mass fraction of triacontanol in the G composition is not more than 0.1%, the stabilizer in the G composition is acetic acid; the mass fraction of the stabilizer in the G composition is 1-3%; the emulsifier in the G composition is fatty alcohol polyoxyethylene ether; the mass fraction of the emulsifier in the G composition is 2-6%; the solvent in the G composition is propylene glycol; the co-solvent in the G composition is dimethyl sulfoxide; the mass fraction of the co-solvent in the G composition is 10-20%;

[0061] Or the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in the G composition is > 1.9% and ≤ 9.8%, the mass fraction of triacontanol in the G composition is > 0.1% and ≤ 0.2%, the stabilizer in the G composition is formic acid; the mass fraction of the stabilizer in the G composition is 6-10%; the emulsifier in the G composition is Tween 80; the mass fraction of the emulsifier in the G composition is 3-7%; the solvent in the G composition is N,N-dimethylformamide; the co-solvent in the G composition is N-methylpyrrolidone; the mass fraction of the co-solvent in the G composition is 30-40%.

[0062] The emulsifier in the E composition can adopt a commercially available product, for example, a product produced by Nanjing Jetrun Technology Co., Ltd., model Ethylan NS-500LQ, which is a non-ionic hydroxyl polyethylene oxide block copolymer, the molar ratio of EO / PO is 1:1.71, the pH is 6.5-7.5, and it has good emulsifying, wetting and dispersing functions.

[0063] The technical scheme adopted in the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of the present application is as follows:

[0064] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine as described above comprises the following steps: uniformly mixing the formula amount of each component to obtain the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine.

[0065] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of the present application is simple to operate, and the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine prepared has good long-lasting foaming property, dilution stability, low-temperature stability and heat storage stability.

[0066] Preferably, the method of uniform mixing comprises the following steps: dissolving the active ingredient in each composition in the co-solvent, and then adding other components and mixing uniformly.

[0067] The technical scheme adopted in the application of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine as a plant growth regulator of the present application is as follows:

[0068] The application of a liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine as a plant growth regulator as described above.

[0069] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present application can effectively promote plant growth as a plant growth regulator.

[0070] Use of the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine as described above in promoting plant growth.

[0071] Preferably, the liquid formulation is the A composition and / or the B composition, and the liquid formulation has the effect of promoting coleoptile growth. Further preferably, the liquid formulation is the A composition and / or the B composition, and the liquid formulation has the effect of promoting coleoptile growth of oat.

[0072] Preferably, the liquid formulation is the C composition and / or the D composition, and the liquid formulation has the effect of increasing plant height and / or increasing the content of a nutrient in plant leaves, the nutrient being selected from one or any combination of chlorophyll, protein and fat. Further preferably, the liquid formulation is the C composition and / or the D composition, and the liquid formulation has the effect of increasing plant height and / or increasing the content of a nutrient in plant leaves, the nutrient being selected from one or any combination of chlorophyll, protein and fat. Preferably, the liquid formulation is the C composition and / or the D composition, and the food is peanut.

[0073] Preferably, the liquid formulation is the E composition and / or the F composition, and the liquid formulation has the effect of increasing fruit setting rate and / or improving fruit quality of a plant, the fruit quality being heavy single fruit and / or vitamin C content in fruit. Further preferably, the liquid formulation is the E composition and / or the F composition, and the liquid formulation has the effect of increasing fruit setting rate and / or improving fruit quality of an apple, the fruit quality being heavy single fruit and / or vitamin C content in fruit.

[0074] Preferably, the liquid formulation is the G composition, and the liquid formulation has the effect of increasing fruit volume and / or weight of a plant. Preferably, the liquid formulation is the G composition, and the liquid formulation has the effect of increasing fruit diameter of a plant. Further preferably, the liquid formulation is the G composition, and the liquid formulation has the effect of increasing longitudinal diameter and / or transverse diameter of a mango fruit. DETAILED DESCRIPTION

[0075] The technical solutions of the present application are further described below in combination with specific examples.

[0076] The pH value of the liquid formulation in Examples 1-8 is tested according to the provisions in standard GB / T 1601;

[0077] The persistent foaming property is tested according to the standard GB / T 28137, and the foam volume at 1 min is recorded. If the foam volume is not more than 40 mL, the persistent foaming property test result is qualified, otherwise, it is unqualified.

[0078] The test method of dilution stability is as follows: 5 mL of the sample (liquid preparation) is taken by a pipette and placed in a 100 mL graduated cylinder, and diluted to 100 mL with standard hard water, and shaken well. The graduated cylinder is placed in a constant temperature water bath at 30±2℃, and left for 1 h. The appearance of the diluted solution in the graduated cylinder is observed. If solid particles are precipitated in the diluted solution, the dilution stability test result is unqualified. If no solid particles are precipitated in the diluted solution, the dilution stability test result is qualified. The standard hard water is prepared according to the standard GB / T 14825.

[0079] The low temperature stability is tested according to the method of "emulsion and homogeneous liquid preparation" in the standard GB / T 19137. The specific method is as follows: 100 mL of the liquid preparation is placed in a beaker, and then the beaker is stored at 0±2℃ for 7 days. Then the beaker is taken out and restored to room temperature. Whether oil is precipitated in the beaker is observed, and the volume of the precipitated oil is measured. If no oil is precipitated or the volume of the precipitated oil is not more than 0.3 mL, the low temperature stability test result is qualified. If the volume of the precipitated oil is more than 0.3 mL, the low temperature stability test result is unqualified.

[0080] The test method of heat storage stability is as follows: 30 mL of the sample (liquid preparation) is measured, and tested according to the method of "liquid preparation" in the standard GB / T 19136. The specific method is as follows: the sample is injected into a clean ampoule by a syringe, and sealed with a high temperature flame. The sealed ampoule is stored in a constant temperature oven at 54±2℃ for 14 days, and then taken out and restored to room temperature. The mass of the sample is measured. If the mass of the sample does not change, the mass fraction of the active ingredient, the pH value of the sample and the dilution stability of the sample are measured within 24 h. If the mass fraction of the active ingredient is not less than 95% of that before heat storage, and the test results of the pH value of the sample and the dilution stability after heat storage are both qualified, the heat storage stability test result is qualified.

[0081] The mass fraction of the active ingredient is tested by liquid chromatography-ultraviolet detector. The liquid chromatography instrument is Agilent 1260 high performance liquid chromatograph, and the ultraviolet instrument is a detector with adjustable ultraviolet wavelength. The chromatographic column is 150 mm×4.6 mm (id) with C18 5 μm filler. The microsyringe is 25 μL. The chromatographic conditions are as follows: the mobile phase is methanol+water+acetic acid=40+60+0.1 (V / V / V), which is ultrasonically degassed and filtered; the flow rate is 1.0 mL / min; the column temperature is 25±2℃; the detection wavelength is 210 nm; and the injection volume is 5 μL.

[0082] Example 1

[0083] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present example is composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine (Anisiflupurin), gibberellic acid, stabilizer, emulsifier, solvent and cosolvent; the types of gibberellic acid, stabilizer, emulsifier, solvent and cosolvent and the mass fraction of each component are shown in Table 1.

[0084] Table 1 Types of gibberellic acid, stabilizer, emulsifier, solvent and cosolvent and mass fraction of each component in the liquid formulation of Example 1

[0085] Material category Composition Mass fraction (%) Effective component Anisiflupurin 0.9 Effective component Gibberellin acid GA3 0.9 Co-solvent Dimethyl sulfoxide 20 Stabilizer Formic acid 1 Emulsifier Octyl phenol polyoxyethylene ether 2 Solvent Ethylene glycol 75.2

[0086] The method for preparing the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present example specifically comprises the following steps: first, use a diaphragm pump to draw the cosolvent into the reaction kettle, turn on the stirring, and the stirring speed is 80 rpm; while stirring, add Anisiflupurin and gibberellic acid; after the addition is complete, continue stirring for 30 min; there are no visible solute particles in the reaction kettle, indicating complete dissolution; then, add the stabilizer and emulsifier in sequence, continue stirring for 60 min, and finally add the solvent, continue stirring for 30 min, to obtain the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine.

[0087] In other embodiments, when preparing the liquid formulation, the stirring speed is controlled to be 40-80 rpm; after the addition of Anisiflupurin and gibberellic acid is complete, the stirring time is controlled to be 30-60 min; after the addition of the stabilizer and emulsifier, the stirring time is controlled to be 30-60 min; and after the addition of the solvent, the stirring time is controlled to be 30-60 min.

[0088] The liquid formulation of the present example was tested for the content of Anisiflupurin and gibberellic acid, pH value, persistent foaming property, dilution stability, low-temperature stability and heat storage stability, and the results are shown in Table 2.

[0089] Table 2 Performance test results of the liquid formulation of Example 1

[0090]

[0091]

[0092] In order to investigate the influence of different cosolvents on liquid preparation, 20 g of cosolvent was added in the mixing device, Anisiflupurin 0.9 g and gibberellic acid GA3 0.9 g were accurately weighed, and then dissolved under the condition of 80 r / min stirring speed for 30 min. The dissolution of Anisiflupurin and gibberellic acid GA3 was observed, and the results are shown in Table 3.

[0093] Table 3 Dissolution of Anisiflupurin and gibberellic acid GA3 in different cosolvents

[0094]

[0095] As shown in Table 3, when the same mass of anhydrous ethanol, cyclohexanone, propylene glycol methyl ether acetate, N,N-dimethylformamide and dimethyl sulfoxide was used to dissolve the raw materials, only N,N-dimethylformamide and dimethyl sulfoxide had the best dissolution effect on Anisiflupurin and gibberellic acid GA3.

[0096] In order to investigate the influence of stabilizers on liquid preparation, the liquid preparation containing different stabilizers was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 1. The types of stabilizers and the dilution stability of each liquid preparation prepared are shown in Table 4.

[0097] Table 4 Types of stabilizers and dilution stability of each liquid preparation prepared

[0098]

[0099] As shown in Table 4, when formic acid was selected as the stabilizer, the dilution stability of the preparation was qualified; when aluminum formate, magnesium formate and citric acid were selected as the stabilizer, the bottom of the liquid preparation appeared precipitate during the test of dilution stability, which was unqualified.

[0100] When the cosolvent in Table 4 was replaced by N,N-dimethylformamide or the emulsifier was replaced by Tween 80, the test results of dilution stability were unqualified.

[0101] Finally, the effect of the amount of each component on the liquid preparation was investigated, and the specific method was as follows: the liquid preparation was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine in Example 1, except that the mass fraction of each component was changed. The results showed that when the mass fraction of Anisiflupurin was ≤0.9%, the mass fraction of gibberellic acid GA3 was ≤0.9%, the mass fraction of the cosolvent was 15-25%, the mass fraction of the stabilizer was 0.5-2%, the mass fraction of the emulsifier was 1-4%, and the balance was the solvent, the prepared liquid preparation was a clear and transparent liquid, and the pH value was 2-5. The test results of the long-lasting foaming property, dilution stability, low-temperature stability, and heat storage stability were all qualified. When the mass fraction of a component in the liquid preparation was not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation did not meet the requirements.

[0102] Example 2

[0103] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of this example was composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine (Anisiflupurin), gibberellic acid, a stabilizer, an emulsifier, a solvent, and a cosolvent. The types of gibberellic acid, the stabilizer, the emulsifier, the solvent, and the cosolvent and the mass fraction of each component are shown in Table 5.

[0104] Table 5 Types of gibberellic acid, the stabilizer, the emulsifier, the solvent, and the cosolvent and the mass fraction of each component in the liquid preparation of Example 2

[0105] Material category Composition Mass fraction (%) Effective component Anisiflupurin 1.8 Effective component Gibberellin acid GA4+7 1.8 Co-solvent N,N-dimethyl formamide 35 Stabilizer Lactic acid 15 Emulsifier Fatty alcohol polyoxyethylene ether 3 Solvent Propylene glycol 43.4

[0106] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of this example specifically included the following steps: first, the cosolvent was pumped into the reaction kettle with a diaphragm pump, and stirring was started with a stirring speed of 40 revolutions / min. Anisiflupurin and gibberellic acid were added while stirring. After the addition was completed, stirring was continued for 60 min, and no visible solute particles were present in the reaction kettle, indicating complete dissolution. Then, the stabilizer and the emulsifier were sequentially added, and stirring was continued for 30 min. Finally, the solvent was added, and stirring was continued for 60 min, to obtain the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine.

[0107] In other embodiments, when preparing the liquid preparation, the stirring speed is controlled to be 40-80 rpm; after the Anisiflupurin and gibberellic acid are added, the stirring time is controlled to be 30-60 min; after the stabilizer and emulsifier are added, the stirring time is controlled to be 30-60 min; and after the solvent is added, the stirring time is controlled to be 30-60 min.

[0108] The liquid preparation of the present embodiment was tested for the content of Anisiflupurin and gibberellic acid, pH value, persistent foaming property, dilution stability, low-temperature stability, and heat storage stability, and the results are shown in Table 6.

[0109] Table 6 Performance test results of the liquid preparation of Example 2

[0110] Item Index Test result Result judgment Mass fraction of Anisiflupurin, % 1.8±0.27 1.87 Pass Mass fraction of Gibberellin acid GA4+7, % 1.8±0.27 1.82 Pass pH value 2-5 3.91 Pass Persistent foaming property (after 1 min), mL ≤ 40 20 Pass Dilution stability Pass Pass Pass Low temperature stability Pass Pass Pass Hot storage stability Pass Pass Pass

[0111] To investigate the effect of different cosolvents on the liquid preparation, 35 g of cosolvent was added in a mixing device, and Anisiflupurin 1.8 g and gibberellic acid GA4+7 1.8 g were accurately weighed and dissolved under the condition of a stirring speed of 40 rpm for 60 min. The dissolution of Anisiflupurin and gibberellic acid GA4+7 was observed, and the results are shown in Table 7.

[0112] Table 7 Dissolution of Anisiflupurin and gibberellic acid GA4+7 with different cosolvents

[0113]

[0114] As shown in Table 7, when the same mass of trimethyl phosphate, monoethanolamine, methyl isobutyl ketone, N-methyl pyrrolidone, and N,N-dimethylformamide is used to dissolve the raw materials, only N-methyl pyrrolidone and N,N-dimethylformamide have the best dissolution effect on Anisiflupurin and gibberellic acid GA4+7.

[0115] To investigate the effect of stabilizers on the liquid preparation, the liquid preparation containing different stabilizers was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 2. The types of stabilizers and the dilution stability of each prepared liquid preparation are shown in Table 8.

[0116] Table 8 Types of stabilizers and dilution stability of each prepared liquid preparation

[0117]

[0118] As shown in Table 8, when lactic acid is selected as the stabilizer, the dilution stability of the preparation is qualified; when aluminum sulfate, iron sulfate or malic acid is selected as the stabilizer, the bottom of the liquid preparation appears precipitate during the test of dilution stability, which is unqualified.

[0119] When the cosolvent in Table 8 is replaced by N-methylpyrrolidone or the emulsifier is replaced by Tween 80, the test results of dilution stability are unqualified.

[0120] Finally, the effect of the amount of each component on the liquid preparation is investigated, and the specific method is as follows: the liquid preparation is prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 2, except that the mass fraction of each component is changed. The results show that when the mass fraction of Anisiflupurin is ≤1.8%, the mass fraction of gibberellic acid GA4+7 is ≤1.8%, the mass fraction of the cosolvent is 30-40%, the mass fraction of the stabilizer is 10-20%, the mass fraction of the emulsifier is 2-4%, and the rest is the solvent, the prepared liquid preparation is a clear and transparent liquid, and the pH value is 2-5. The test results of long-lasting foaming property, dilution stability, low-temperature stability and heat storage stability are all qualified. When the mass fraction of a component in the liquid preparation is not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation do not meet the requirements.

[0121] Example 3

[0122] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present example is composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine (Anisiflupurin), brassinolide, a stabilizer, an emulsifier, a solvent and a cosolvent; the types of brassinolide, stabilizer, emulsifier, solvent and cosolvent and the mass fraction of each component are shown in Table 9.

[0123] Table 9 Types of brassinolide, stabilizer, emulsifier, solvent and cosolvent in the liquid preparation of Example 3 and the mass fraction of each component

[0124] Material category Composition Mass fraction (%) Effective component Anisiflupurin 1.99 Effective component 24-epibrassinolide 0.01 Co-solvent N-methyl pyrrolidone 15 Stabilizer Glacial acetic acid 5 Emulsifier Tween 80 5 Solvent Propylene glycol 73

[0125] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of the embodiment specifically comprises the following steps: first, use a diaphragm pump to draw the cosolvent into the reaction kettle, start stirring, the stirring speed is 80 rpm, add Anisiflupurin, brassinolide while stirring, after the addition is completed, continue stirring for 30 min, there are no visible solute particles in the reaction kettle, achieving complete dissolution; then, add the stabilizer and the emulsifier in turn, continue stirring for 60 min, and finally add the solvent, continue stirring for 30 min, to obtain the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine.

[0126] In other embodiments, when preparing the liquid preparation, the stirring speed is controlled to be 40-80 rpm; after the addition of Anisiflupurin and brassinolide is completed, the stirring time is controlled to be 30-60 min; after the addition of the stabilizer and the emulsifier, the stirring time is controlled to be 30-60 min; and after the addition of the solvent, the stirring time is controlled to be 30-60 min.

[0127] The liquid preparation of the embodiment is tested for the content of Anisiflupurin and brassinolide, pH value, persistent foaming property, dilution stability, low-temperature stability, and heat storage stability, and the results are shown in Table 10.

[0128] Table 10 Performance test results of the liquid preparation of Example 3

[0129] Item Index Test result Result judgment Mass fraction of Anisiflupurin, % 1.99±0.2985 2.01 Pass Mass fraction of 24-epibrassinolide, % 0.01±0.0015 0.0101 Pass pH value 2-5 4.37 Pass Persistent foaming property (after 1 min), mL ≤ 40 16 Pass Dilution stability Pass Pass Pass Low temperature stability Pass Pass Pass Hot storage stability Pass Pass Pass

[0130] In order to investigate the influence of different cosolvents on the liquid preparation, 15 g of cosolvent is added in a mixing device, Anisiflupurin 1.99 g and 24-epibrassinolide 0.01 g are accurately weighed, and the stirring and dissolution are performed at a speed of 80 rpm for 30 min, and the dissolution of Anisiflupurin and 24-epibrassinolide is observed, and the results are shown in Table 11.

[0131] Table 11 Dissolution of Anisiflupurin and 24-epibrassinolide with different cosolvents

[0132]

[0133] As shown in Table 11, when the same mass of triethanolamine, n-butyl ether, ethyl acetate, ethylene glycol, and N-methyl pyrrolidone is used to dissolve the raw materials, only ethylene glycol and N-methyl pyrrolidone have the best dissolution effect on Anisiflupurin and 24-epibrassinolide.

[0134] To investigate the effect of stabilizer on the liquid preparation, the liquid preparation containing different stabilizers was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 3, the type of stabilizer and the dilution stability of each prepared liquid preparation were shown in Table 12.

[0135] Table 12 Type of stabilizer and dilution stability of each prepared liquid preparation

[0136]

[0137] It can be seen from Table 12 that when glacial acetic acid is selected as the stabilizer, the dilution stability of the preparation is qualified; when ammonia, 0.1 mol / L NaOH aqueous solution or tartaric acid is selected as the stabilizer, the bottom of the liquid preparation appears precipitate during the test of dilution stability, which is unqualified.

[0138] When the cosolvent in Table 12 is replaced by ethylene glycol or the emulsifier is replaced by Span 60, the test results of dilution stability are unqualified.

[0139] Finally, the effect of the amount of each component on the liquid preparation was investigated, and the specific method was as follows: the liquid preparation was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 3, the difference was that the mass fraction of each component was changed, and the results showed that when the mass fraction of Anisiflupurin was ≤1.99%, the mass fraction of 24-homo brassinolide was ≤0.01%, the mass fraction of cosolvent was 10-20%, the mass fraction of stabilizer was 3-6%, the mass fraction of emulsifier was 3-7%, and the balance was solvent, the prepared liquid preparation was a clear and transparent liquid, and the pH value was 2-5, the test results of persistent foaming property, dilution stability, low temperature stability and heat storage stability were qualified. When the mass fraction of a component in the liquid preparation was not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation did not meet the requirements.

[0140] Example 4

[0141] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present example is composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine (Anisiflupurin), brassinolide, stabilizer, emulsifier, solvent and cosolvent; the types of brassinolide, stabilizer, emulsifier, solvent and cosolvent and the mass fraction of each component are shown in Table 13.

[0142] Table 13 Types of brassinolide, stabilizer, emulsifier, solvent and cosolvent and mass fraction of each component in the liquid formulation of Example 4

[0143] Material category Composition Mass fraction (%) Effective component Anisiflupurin 4.995 Effective component 28-homobrassinolide 0.005 Co-solvent Dimethyl sulfoxide 30 Stabilizer Formic acid 0.5 Emulsifier Polyethylene glycol 400 6 Solvent N,N-dimethyl formamide 58.5

[0144] The preparation method of the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of the present embodiment specifically comprises the following steps: first, use a diaphragm pump to draw the cosolvent into the reaction kettle, turn on the stirring, and the stirring speed is 40 revolutions / min; while stirring, add Anisiflupurin and brassinolide; after the addition is complete, continue stirring for 60 min; there are no visible solute particles in the reaction kettle, achieving complete dissolution; then, add the stabilizer and emulsifier in sequence, continue stirring for 30 min, and finally add the solvent, continue stirring for 60 min, to obtain the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine.

[0145] In other embodiments, when preparing the liquid formulation, the stirring speed is controlled to be 40-80 revolutions / min; after the addition of Anisiflupurin and brassinolide is complete, the stirring time is controlled to be 30-60 min; after the addition of the stabilizer and emulsifier, the stirring time is controlled to be 30-60 min; and after the addition of the solvent, the stirring time is controlled to be 30-60 min.

[0146] The liquid formulation of the present embodiment is tested for the content of Anisiflupurin and brassinolide, pH value, persistent foaming property, dilution stability, low-temperature stability and heat storage stability, and the results are shown in Table 14.

[0147] Table 14 Performance test results of the liquid formulation of Example 4

[0148] Item Index Test result Result judgment Mass fraction of Anisiflupurin, % 4.995±0.4995 4.990 Pass Mass fraction of 28-homobrassinolide, % 0.005±0.00075 0.0049 Pass pH value 2-5 3.91 Pass Persistent foaming property (after 1 min), mL ≤ 40 13 Pass Dilution stability Pass Pass Pass Low temperature stability Pass Pass Pass Hot storage stability Pass Pass Pass

[0149] In order to investigate the influence of different cosolvents on the liquid formulation, 30 g of cosolvent is added in a mixing device, Anisiflupurin 4.995 g and 28-homobrassinolide 0.005 g are accurately weighed, and stirred and dissolved at a stirring speed of 40 revolutions / min for 60 min, and the dissolution of Anisiflupurin and 28-homobrassinolide is observed, and the results are shown in Table 15.

[0150] Table 15 Dissolution of Anisiflupurin and 28-homobrassinolide with different cosolvents

[0151]

[0152]

[0153] As shown in Table 15, when the same amount of anhydrous ethanol, n-butanol, ethyl acetate, propylene glycol and dimethyl sulfoxide is used to dissolve the raw material, only propylene glycol and dimethyl sulfoxide have the best solubility for Anisiflupurin and 28-homobrassinolide.

[0154] To investigate the effect of stabilizers on the liquid preparation, the liquid preparation containing different stabilizers was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 4, and the type of stabilizer and the dilution stability of each prepared liquid preparation are shown in Table 16.

[0155] Table 16 Type of stabilizer and dilution stability of each prepared liquid preparation

[0156]

[0157] As shown in Table 16, when formic acid is selected as the stabilizer, the dilution stability of the preparation is qualified; when aluminum formate, magnesium formate and propionic acid are selected as the stabilizer, the bottom of the liquid preparation appears precipitate during the test of dilution stability, which is unqualified.

[0158] When the cosolvent in Table 16 is replaced by propylene glycol or the emulsifier is replaced by Span 80, the test results of dilution stability are unqualified.

[0159] Finally, the effect of the amount of each component on the liquid preparation was investigated, and the specific method is as follows: the liquid preparation was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 4, the difference is that the mass fraction of each component is changed, and the results show that when the mass fraction of Anisiflupurin is ≤4.995%, the mass fraction of 28-homobrassinolide is ≤0.005%, the mass fraction of the cosolvent is 20-40%, the mass fraction of the stabilizer is 0.3-0.6%, the mass fraction of the emulsifier is 4-8%, and the rest is the solvent, the prepared liquid preparation is a clear and transparent liquid, and the pH value is 2-5, the test results of the long-lasting foaming property, dilution stability, low-temperature stability and heat storage stability are qualified. When the mass fraction of a component in the liquid preparation is not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation do not meet the requirements.

[0160] Example 5

[0161] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present embodiment is composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine (Anisiflupurin), metaldehyde, stabilizer, emulsifier, solvent and cosolvent; the types of stabilizer, emulsifier, solvent and cosolvent and the mass fractions of the components are shown in Table 17. The manufacturer of the EO / PO block polyether in Table 17 is Nanjing Jetrun Technology Co., Ltd., the product model is Ethylan NS-500LQ, and the molar ratio of EO / PO in the EO / PO block polyether is 1:1.71.

[0162] Table 17 Types of stabilizer, emulsifier, solvent and cosolvent in the liquid preparation of Example 5 and mass fractions of the components

[0163] Material category Composition Mass fraction (%) Effective component Anisiflupurin 2 Effective component Milneb 8 Co-solvent N-methyl pyrrolidone 15 Stabilizer BHT (2,6-di-tert-butyl-p-cresol) 2 Emulsifier EO / PO block polyether 1 Solvent N,N-dimethyl formamide 72

[0164] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present embodiment specifically comprises the following steps: first, use a diaphragm pump to draw the cosolvent into the reaction kettle, start stirring, the stirring speed is 80 revolutions / min, add Anisiflupurin and metaldehyde while stirring, after the addition is completed, continue stirring for 30 min, there are no visible solute particles in the reaction kettle, achieving complete dissolution; then, add the stabilizer and the emulsifier in turn, continue stirring for 60 min, and finally add the solvent, continue stirring for 30 min, to obtain the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine.

[0165] In other embodiments, when preparing the liquid preparation, the stirring speed is controlled to be 40-80 revolutions / min; after the addition of Anisiflupurin and metaldehyde is completed, the stirring time is controlled to be 30-60 min; after the addition of the stabilizer and the emulsifier, the stirring time is controlled to be 30-60 min; and after the addition of the solvent, the stirring time is controlled to be 30-60 min.

[0166] The liquid preparation of the present embodiment is tested for the content of Anisiflupurin and metaldehyde, pH value, persistent foaming property, dilution stability, low-temperature stability and heat storage stability, and the results are shown in Table 18.

[0167] Table 18 Performance test results of the liquid preparation of Example 5

[0168] Item Index Test result Result judgment Mass fraction of Anisiflupurin, % 2.0±0.3 2.1 Pass Mass fraction of Milneb, % 8±0.8 7.9 Pass pH value 5.0-8.0 7.52 Pass Persistent foaming property (after 1 min), mL ≤ 40 18 Pass Dilution stability Pass Pass Pass Low temperature stability Pass Pass Pass Hot storage stability Pass Pass Pass

[0169] In order to investigate the influence of different cosolvents on the liquid preparation, 15 g of cosolvent was added in the mixing device, Anisiflupurin 2.00 g and amaranth 8.00 g were accurately weighed, and then dissolved under the condition of 80 r / min for 30 min. The dissolution of Anisiflupurin and amaranth was observed, and the results are shown in Table 19.

[0170] Table 19 Dissolution of Anisiflupurin and amaranth in different cosolvents

[0171]

[0172] As shown in Table 19, when the same mass of trimethyl phosphate, monoethanolamine, methyl isobutyl ketone, ethylene glycol and N-methyl pyrrolidone was used to dissolve the raw materials, only ethylene glycol and N-methyl pyrrolidone had the best dissolution effect on Anisiflupurin and amaranth.

[0173] In order to investigate the influence of stabilizers on the liquid preparation, the liquid preparation containing different stabilizers was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 5. The types of stabilizers and the dilution stability of each prepared liquid preparation are shown in Table 20. BHT in Table 20 represents 2,6-di-tert-butyl-p-cresol, TBHQ represents tert-butyl hydroquinone, and the manufacturer of EO / PO block polyether is Nanjing Jetrun Technology Co., Ltd., and the product model is Ethylan NS-500LQ.

[0174] Table 20 Types of stabilizers and dilution stability of each prepared liquid preparation

[0175]

[0176] As shown in Table 20, when BHT or TBHQ is selected as the stabilizer, the dilution stability of the preparation is qualified; when iron sulfate, ammonia and tea polyphenol are selected as the stabilizer, the bottom of the liquid preparation appears precipitate during the test of dilution stability, which is unqualified.

[0177] When the cosolvent in Table 20 is replaced by ethylene glycol or the emulsifier is replaced by Tween 80, the test results of dilution stability are unqualified.

[0178] Finally, the effect of the amount of each component on the liquid preparation is investigated, and the specific method is as follows: the liquid preparation is prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 5, except that the mass fraction of each component is changed. The results show that when the mass fraction of Anisiflupurin is ≤2%, the mass fraction of the amyl ester is ≤8%, the mass fraction of the cosolvent is 20-30%, the mass fraction of the stabilizer is 1-3%, the mass fraction of the emulsifier is 0.5-2%, and the balance is the solvent, the prepared liquid preparation is a clear and transparent liquid, and the pH value is 2-5. The test results of the long-lasting foaming property, dilution stability, low-temperature stability, and heat storage stability are all qualified. When the mass fraction of a component in the liquid preparation is not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation do not meet the requirements.

[0179] Example 6

[0180] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of this example is composed of the following components with the following mass fractions: 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine (Anisiflupurin), ethephon, emulsifier, solvent, and cosolvent; the types of the emulsifier, solvent, and cosolvent and the mass fractions of each component are shown in Table 21.

[0181] Table 21 Types of emulsifier, solvent, and cosolvent and mass fractions of each component in the liquid preparation of Example 6

[0182] Material category Composition Mass fraction (%) Effective component Anisiflupurin 0.5 Effective component Ethylene 29.5 Co-solvent Lactic acid 35 Emulsifier Polyethylene glycol 400 5 Solvent Deionized water 30

[0183] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of this example specifically includes the following steps: first, use a diaphragm pump to draw the cosolvent into the reaction kettle, start stirring, and the stirring speed is 80 revolutions / min. Anisiflupurin and ethephon are added while stirring. After the addition is completed, continue stirring for 30 min, and there are no visible solute particles in the reaction kettle, achieving complete dissolution. Then, the emulsifier is added in sequence, and continue stirring for 60 min. Finally, the solvent is added, and continue stirring for 30 min to obtain the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine.

[0184] In other examples, when preparing the liquid preparation, the stirring speed is controlled to be 40-80 revolutions / min. After the addition of Anisiflupurin and ethephon is completed, the stirring time is controlled to be 30-60 min. After the addition of the emulsifier, the stirring time is controlled to be 30-60 min. After the addition of the solvent, the stirring time is controlled to be 30-60 min.

[0185] The liquid preparation of the present example was tested for Anisiflupurin, ethephon content, pH value, persistent foaming property, dilution stability, low temperature stability and heat storage stability, and the results are shown in Table 22.

[0186] Table 22 Test results of performance of the liquid preparation of Example 6

[0187] Item Index Test result Result judgment Mass fraction of Anisiflupurin, % 0.5±0.075 0.506 Pass Mass fraction of Ethylene, % 29.5±1.475 29.8 Pass pH value 2.0-5.0 2.38 Pass Persistent foaming property (after 1 min), mL ≤ 40 10 Pass Dilution stability Pass Pass Pass Low temperature stability Pass Pass Pass Hot storage stability Pass Pass Pass

[0188] To investigate the effect of different cosolvents on the liquid preparation, 35 g of cosolvent was added in the mixing device, and 0.5 g of Anisiflupurin and 29.5 g of ethephon were accurately weighed, and stirred and dissolved at a rotation speed of 80 r / min for 30 min. The dissolution of Anisiflupurin and ethephon was observed, and the results are shown in Table 23.

[0189] Table 23 Dissolution of Anisiflupurin and ethephon with different cosolvents

[0190]

[0191] As shown in Table 23, when the same mass of anhydrous ethanol, n-butanol, ethyl acetate, propionic acid and lactic acid was used to dissolve the raw materials, only propionic acid and lactic acid had the best dissolution effect on Anisiflupurin and ethephon.

[0192] To investigate the effect of solvent on the liquid preparation, the liquid preparation containing different solvents was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 6. The types of solvents and the dilution stability of each liquid preparation prepared are shown in Table 24.

[0193] Table 24 Types of solvents and dilution stability of each liquid preparation prepared

[0194] Material category Composition Mass fraction (%) Mass fraction (%) Mass fraction (%) Active ingredient Anisiflupurin 0.5 0.5 0.5 Active ingredient Ethylene glycol 29.5 29.5 29.5 Co-solvent Lactic acid 35 35 35 Emulsifier Polyethylene glycol 400 5 5 5 Solvent Ethylene glycol 30 - - Solvent Propylene glycol - 30 - Solvent Deionized water - - 30 Dilution stability - Pass Pass Pass

[0195] As shown in Table 24, when ethylene glycol, propylene glycol and deionized water were selected as solvents, the dilution stability of the preparation was qualified; however, the cost of deionized water was lower.

[0196] When the cosolvent in Table 24 was replaced by propionic acid instead of lactic acid, or the emulsifier was replaced by Tween 80 instead of polyethylene glycol 400, the test results of dilution stability were unqualified.

[0197] Finally, the effect of the amount of each component on the liquid preparation is investigated, and the specific method is as follows: the liquid preparation is prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 6, except that the mass fraction of each component is changed. The results show that when the mass fraction of Anisiflupurin is ≤0.5%, the mass fraction of ethephon is ≤29.5%, the mass fraction of the cosolvent is 30-40%, the mass fraction of the emulsifier is 3-6%, and the balance is the solvent, the prepared liquid preparation is a clear and transparent liquid, and the pH value is 2-5. The test results of the long-lasting foaming property, dilution stability, low-temperature stability, and heat storage stability are all qualified. When the mass fraction of a component in the liquid preparation is not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation do not meet the requirements.

[0198] Example 7

[0199] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of this example is composed of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine (Anisiflupurin), triacontanol, a stabilizer, an emulsifier, a solvent, and a cosolvent. The types of the stabilizer, the emulsifier, the solvent, and the cosolvent and the mass fraction of each component are shown in Table 25.

[0200] Table 25 Types of stabilizer, emulsifier, solvent, and cosolvent and mass fraction of each component in the liquid preparation of Example 7

[0201] Material category Composition Mass fraction (%) Active ingredient Anisiflupurin 1.9 Active ingredient Tricosanol 0.1 Co-solvent Dimethyl sulfoxide 15 Stabilizer Glacial acetic acid 2 Emulsifier Fatty alcohol polyoxyethylene ether 4 Solvent Propylene glycol 77

[0202] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of this example specifically includes the following steps: first, the cosolvent is pumped into the reaction kettle with a diaphragm pump, the stirring is started, the stirring speed is 80 rpm, Anisiflupurin and triacontanol are added while stirring, after the addition is completed, the stirring is continued for 30 min, and there are no visible solute particles in the reaction kettle, achieving complete dissolution; then the stabilizer and the emulsifier are sequentially added, and the stirring is continued for 60 min; finally, the solvent is added, and the stirring is continued for 30 min, to obtain the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine.

[0203] In other examples, when preparing the liquid preparation, the stirring speed is controlled to be 40-80 rpm; after the addition of Anisiflupurin and triacontanol is completed, the stirring time is controlled to be 30-60 min; after the addition of the stabilizer and the emulsifier, the stirring time is controlled to be 30-60 min; and after the addition of the solvent, the stirring time is controlled to be 30-60 min.

[0204] The liquid preparation of the present example was tested for Anisiflupurin, triacontanol content, pH value, persistent foaming property, dilution stability, low temperature stability and heat storage stability, and the results are shown in Table 26.

[0205] Table 26 Performance test results of the liquid preparation of Example 7

[0206] Item Index Test result Result judgment Mass fraction of Anisiflupurin, % 1.9±0.285 1.931 Pass Mass fraction of Tricosanol, % 0.1±0.015 0.105 Pass pH value 2.0-5.0 3.68 Pass Persistent foaming property (after 1 min), mL ≤ 40 24 Pass Dilution stability Pass Pass Pass Low-temperature stability Pass Pass Pass Thermal storage stability Pass Pass Pass

[0207] To investigate the effect of different cosolvents on the liquid preparation, 15 g of cosolvent was added in the mixing device, and Anisiflupurin 1.9 g and triacontanol 0.1 g were accurately weighed. Under the condition of 80 rpm, the dissolution of Anisiflupurin and triacontanol was observed after stirring for 30 min, and the results are shown in Table 27.

[0208] Table 27 Solubility of Anisiflupurin and triacontanol with different cosolvents

[0209]

[0210] As shown in Table 27, when the same mass of trimethyl phosphate, monoethanolamine, methyl isobutyl ketone, ethylene glycol and dimethyl sulfoxide was used to dissolve the raw materials, only ethylene glycol and dimethyl sulfoxide had the best solubility effect on Anisiflupurin and triacontanol.

[0211] To investigate the effect of stabilizers on the liquid preparation, the liquid preparation containing different stabilizers was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 7. The type of stabilizer and the dilution stability of each liquid preparation prepared are shown in Table 28.

[0212] Table 28 Type of stabilizer and dilution stability of each liquid preparation prepared

[0213]

[0214]

[0215] As shown in Table 28, when glacial acetic acid was selected as the stabilizer, the dilution stability of the preparation was qualified; when iron sulfate, ammonia and lactic acid were selected as the stabilizer, precipitates appeared at the bottom of the liquid preparation during the dilution stability test, which was unqualified.

[0216] When the cosolvent in Table 28 was replaced by ethylene glycol or the emulsifier was replaced by octylphenol polyoxyethylene ether, the test results of dilution stability were unqualified.

[0217] Finally, the effect of the amount of each component on the liquid preparation was investigated, and the specific method was as follows: the liquid preparation was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 7, except that the mass fraction of each component was changed. The results showed that when the mass fraction of Anisiflupurin was ≤1.9%, the mass fraction of triacontanol was ≤0.1%, the mass fraction of the cosolvent was 10-20%, the mass fraction of the stabilizer was 1-3%, the mass fraction of the emulsifier was 2-6%, and the balance was the solvent, the prepared liquid preparation was a clear and transparent liquid, and the pH value was 2-5. The test results of the long-lasting foaming property, dilution stability, low-temperature stability, and heat storage stability were all qualified. When the mass fraction of a component in the liquid preparation was not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation did not meet the requirements.

[0218] Example 8

[0219] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of this example was composed of the following mass fractions of components: 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine (Anisiflupurin), triacontanol, a stabilizer, an emulsifier, a solvent, and a cosolvent; the types of the stabilizer, the emulsifier, the solvent, and the cosolvent and the mass fractions of the components are shown in Table 29.

[0220] Table 29 Types of stabilizers, emulsifiers, solvents, and cosolvents and mass fractions of components in the liquid preparation of Example 8

[0221] Material category Composition Mass fraction (%) Active ingredient Anisiflupurin 9.8 Active ingredient Tricosanol 0.2 Co-solvent N-methyl pyrrolidone 35 Stabilizer Formic acid 8 Emulsifier Tween 80 5 Solvent N,N-dimethylformamide 42

[0222] The preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of this example specifically included the following steps: first, the cosolvent was pumped into the reaction kettle with a diaphragm pump, the stirring was started, the stirring speed was 40 revolutions / min, Anisiflupurin and triacontanol were added while stirring, after the addition was completed, the stirring was continued for 60 min, and there were no visible solute particles in the reaction kettle, achieving complete dissolution; then the stabilizer and the emulsifier were sequentially added, the stirring was continued for 30 min, and finally the solvent was added, the stirring was continued for 60 min, and the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine was obtained.

[0223] In other embodiments, when preparing the liquid preparation, the stirring speed is controlled to be 40-80 rpm; after the addition of Anisiflupurin and triacontanol is completed, the stirring time is controlled to be 30-60 min; after the addition of the stabilizer and the emulsifier, the stirring time is controlled to be 30-60 min; and after the addition of the solvent, the stirring time is controlled to be 30-60 min.

[0224] The liquid preparation of the present example was tested for the content of Anisiflupurin and triacontanol, pH value, persistent foaming property, dilution stability, low-temperature stability, and heat storage stability, and the results are shown in Table 30.

[0225] Table 30 Test results of the performance of the liquid preparation of Example 8

[0226]

[0227]

[0228] To investigate the effect of different cosolvents on the liquid preparation, 35 g of a cosolvent was added in a mixing device, Anisiflupurin 9.8 g and triacontanol 0.2 g were accurately weighed, and the stirring and dissolution were performed at a speed of 40 rpm for 60 min. The dissolution of Anisiflupurin and triacontanol was observed, and the results are shown in Table 31.

[0229] Table 31 Dissolution of Anisiflupurin and triacontanol with different cosolvents

[0230]

[0231] As shown in Table 31, when the same mass of n-butanol, triethanolamine, propylene carbonate, propylene glycol, and N-methyl pyrrolidone is used to dissolve the raw materials, only propylene glycol and N-methyl pyrrolidone have the best dissolution effect on Anisiflupurin and triacontanol.

[0232] To investigate the effect of stabilizers on the liquid preparation, the liquid preparation containing different stabilizers was prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 8. The types of stabilizers and the dilution stability of each prepared liquid preparation are shown in Table 32.

[0233] Table 32 Types of stabilizers and dilution stability of each prepared liquid preparation

[0234]

[0235] As can be seen from Table 32, when formic acid is selected as the stabilizer, the dilution stability of the preparation is qualified; when aluminum formate, magnesium formate or malic acid is selected as the stabilizer, the bottom of the liquid preparation appears precipitate during the test of dilution stability, which is unqualified.

[0236] When the cosolvent in Table 32 is replaced by propylene glycol or the emulsifier is replaced by Span 80, the test results of dilution stability are unqualified.

[0237] Finally, the effect of the amount of each component on the liquid preparation is investigated, and the specific method is as follows: the liquid preparation is prepared according to the preparation method of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in Example 8, except that the mass fraction of each component is changed. The results show that when the mass fraction of Anisiflupurin is >1.9% and ≤9.8%, the mass fraction of triacontanol is >0.1% and ≤0.2%, the mass fraction of the cosolvent is 30-40%, the mass fraction of the stabilizer is 6-10%, the mass fraction of the emulsifier is 3-7%, and the balance is the solvent, the prepared liquid preparation is a clear and transparent liquid, and the pH value is 2-5, and the test results of long-lasting foaming property, dilution stability, low-temperature stability and heat storage stability are all qualified. When the mass fraction of a component in the liquid preparation is not within the above numerical range, one or more of the performance indicators of the prepared liquid preparation do not meet the requirements.

[0238] Comparative Example 1

[0239] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is only different from the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 1 in that the mass fraction of gibberellic acid GA3 in the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0240] Comparative Example 2

[0241] The liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is only different from the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 2 in that the mass fraction of gibberellic acid GA4+7 in the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0242] Comparative Example 3

[0243] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 3 only in that the mass fraction of 24-epibrassinolide in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0244] Comparative Example 4

[0245] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 4 only in that the mass fraction of 28-homobrassinolide in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0246] Comparative Example 5

[0247] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 5 only in that the mass fraction of irgasol in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0248] Comparative Example 6

[0249] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 6 only in that the mass fraction of ethephon in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0250] Comparative Example 7

[0251] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 5 only in that the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0252] Comparative Example 8

[0253] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 6 only in that the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0254] Comparative Example 9

[0255] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 7 only in that the mass fraction of triacontanol in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0256] Comparative Example 10

[0257] The liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example differs from the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 8 only in that the mass fraction of triacontanol in the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of the present comparative example is 0.

[0258] Experimental Example 1

[0259] In order to evaluate the effects of the liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 1 and Example 2 on the growth of oat coleoptile, a commercially available 4% gibberellic acid soluble liquid agent (produced by Zhengzhou Zhengshi Chemical Product Co., Ltd.) was used as a control agent, and water was used as a blank control, and then the different formulations were diluted with water to obtain the test agents. Then the effects of each test agent on the growth of oat coleoptile were tested, and the test method was as follows: oat was cultured in the dark, and when the oat seedlings grew to about 5 cm, the coleoptile was cut from the oat seedlings, and then the top of the coleoptile was cut off (the length of the cut-off was 6 mm) to obtain the top-removed coleoptile. Then a quantitative cutting knife was used to cut a 1 cm long section from the uppermost end of the top-removed coleoptile to obtain the coleoptile section. Then the coleoptile section was soaked in a 2% (mass fraction) sucrose-containing phosphoric acid-citric acid buffer (pH = 5.0) for 3 h to wash away the endogenous auxin. Then washed and dried culture dishes were taken, 10 endogenous auxin-washed coleoptile sections were placed in each culture dish, and the same test agent (20 mL in volume) was added to each culture dish to soak the coleoptile sections in the test agent. At the same time, 5 parallel experiments were set for each test agent (i.e. the number of culture dishes corresponding to each test agent was 5). Then the culture dishes with the test agent and the coleoptile sections were placed in a shaking bed and cultured in the dark for 24 h or 48 h. After the culture ended, the growth of each coleoptile section in each culture dish was tested, and then the average value of the growth of all coleoptile sections in the 5 culture dishes corresponding to each test agent was calculated to obtain the test result of the coleoptile section growth corresponding to the corresponding test agent. The test result of the coleoptile section growth corresponding to the test agent using water was defined as M. Then the coleoptile growth promotion rate corresponding to each test agent was calculated, and the calculation formula was: coleoptile growth promotion rate (%) = (test result of coleoptile section growth-test result of M) / M x 100. The numbers of each test agent, the concentrations of the active ingredients (2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine, gibberellic acid GA3 and gibberellic acid GA4+7) in each test agent, and the coleoptile growth promotion rates corresponding to each test agent at different culture times are shown in Table 33.

[0260] Table 33 Numbers of each test agent, concentrations of active ingredients in each test agent, and coleoptile growth promotion rates corresponding to each test agent at different culture times

[0261]

[0262]

[0263] As shown in Table 33, the liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Examples 1-2 all have the effect of promoting the growth of plumule sheath, and are superior to the promotion of the growth of plumule sheath by the control agent (conventional plant regulator) gibberellic acid.

[0264] Experimental Example 2

[0265] In order to evaluate the effects of the liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Examples 3 and 4 on the growth of crops, commercially available 0.01% 24-epibrassinolide soluble liquid (produced by Zhengzhou Zhengshi Chemical Product Co., Ltd.) and commercially available 0.01% 28-homobrassinolide soluble liquid (produced by Zhengzhou Zhengshi Chemical Product Co., Ltd.) were used as control agent 1 and control agent 2, respectively, and water was used as a blank control. Then, different formulations were diluted with water to obtain test reagents. Then, the effects of each test reagent on the growth of peanuts were tested, and the test method was as follows: peanuts with consistent growth (peanuts in the peanut field were all in the seedling stage) were selected, and the area was randomly divided. Each subarea covered three rows of peanuts, and a row of peanuts was set as a protective row between different subareas. The area of each subarea was 30 m 2 , and a signboard was placed in each subarea. Then, different test reagents were uniformly sprayed on the peanut plants in different subareas in the form of spraying by using an electric sprayer. The number of subareas corresponding to each test reagent was 1, and the mass of liquid formulation sprayed on each peanut plant in each subarea was the same, and the spraying method was also the same. Finally, the height, chlorophyll content, protein content, and fat content of peanut plants at 7 d after spraying were tested. Among them, the test methods of the height, chlorophyll content, protein content, and fat content of peanut plants were as follows:

[0266] (1) Height: 10 peanut plants at different positions in each subarea were randomly selected as sampling points, and a signboard was hung for marking. In order to ensure the accuracy and representativeness of the data, the height of the main stem of the peanut was uniformly measured, the distance between the root and the growing point at the stem tip was measured by using a steel tape, and the distance was the height of the main stem of the peanut plant. The average height of the main stem of the 10 peanut plants randomly selected in each subarea was taken as the test result of the height of the main stem of the peanut plant in the subarea.

[0267] (2) Chlorophyll content: 5 peanut plants at different positions in each sub-area were randomly selected as sampling points and marked with a sign. The chlorophyll content, protein content and fat content of 2 leaves in all leaves except new leaves of the upper layer of each sampling point were randomly determined. The average value of the chlorophyll content of the 2 leaves corresponding to each sampling point was taken as the representative value of the chlorophyll level of the peanut plant at the sampling point, and the testing instrument for chlorophyll content was Konica Minolta SPAD502 handheld chlorophyll meter; the average value of the protein content of the 2 leaves corresponding to each sampling point was taken as the representative value of the protein level of the peanut plant at the sampling point, and the protein content was determined by using a full-automatic Kjeldahl nitrogen determination instrument; the average value of the fat content of the 2 leaves corresponding to each sampling point was taken as the representative value of the fat level of the peanut plant at the sampling point, and the fat content was determined by using a fat determination instrument. Finally, the average value of the representative value of the chlorophyll level, the average value of the representative value of the protein level and the average value of the representative value of the fat level of the 5 peanut plants at different positions in each sub-area were calculated, and the calculated average values were taken as the test results of the chlorophyll content, the test results of the protein content and the test results of the fat content of the peanut plants in the sub-area, respectively.

[0268] The number of each test reagent, the concentration of the active ingredient (2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine, 24-epibrassinolid and 28-homobrassinolid) in each test reagent, and the test results of the plant height, chlorophyll content, protein content and fat content of the peanut after using each test reagent are shown in Table 34.

[0269] Table 34 Number of each test reagent, concentration of active ingredient in each test reagent, and test results of plant height, chlorophyll content, protein content and fat content of peanut after using each test reagent

[0270]

[0271]

[0272] As can be seen from Table 34, the liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purine-6-amine of Examples 3-4 all have the effect of promoting the growth of peanut plants, and compared with the blank control group (water), the liquid formulations of Examples 3-4 can significantly increase the chlorophyll content, protein content and fat content in the leaves of peanut plants, can significantly promote the growth of peanuts, increase the accumulation of chlorophyll, thereby facilitating the accumulation of photosynthetic products, promoting full fruit, increasing yield and quality.

[0273] Experimental Example 3

[0274] In order to evaluate the influence of the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 5 and Example 6 on the growth of crops, a commercially available 30% of Freshcut · Ethylene agent (produced by Zhengzhou Zhengshi Chemical Product Co., Ltd.) was used as a control agent, and water was used as a blank control. Then, the different formulations were diluted with water to obtain the test reagents. Then, the same method in the standard GB / T 17980.145-2004 "Guidelines for Pesticide Field Test (II)" was used to test the Fuji apple with the same growth. The test reagents were uniformly sprayed on the stems and leaves of the apple plants at the fruit setting period and fruit swelling period. The area of the apple plants sprayed with each test reagent was 1 mu, and the mass of the test reagent sprayed on each apple plant was the same each time. After spraying the test reagent each time, the drug resistance was investigated on the 3rd day, and the fruit setting rate, single fruit weight, quality and other data were also investigated. The content of vitamin C in fresh fruit and the hardness of apple fruit were also tested. Five test samples were randomly selected from all the apple plants sprayed with each test reagent, and the average value of the test results of the five test samples was used as the test results of the fruit setting rate, single fruit weight, content of vitamin C in fresh fruit and hardness of apple fruit of the apple after using the corresponding test reagent.

[0275] The number of each test reagent, the concentration of the active ingredient (2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine, Freshcut and ethylene) in each test reagent and the test results of the fruit setting rate, single fruit weight, content of vitamin C in fresh fruit and hardness of apple fruit of the apple after using each test reagent are shown in Table 35.

[0276] Table 35 Number of each test reagent, concentration of active ingredient in each test reagent and corresponding plumule sheath growth rate of each test reagent at different culture times

[0277]

[0278] As can be seen from Table 35, after the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 5-6 was sprayed on the apple trees, the fruit setting rate of the apple was improved, the weight of the single fruit was increased, and the content of vitamin C in the fruit was also improved.

[0279] Experimental Example 4

[0280] In order to evaluate the effect of the liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Example 7 and Example 8 on the growth of crops, a commercially available 0.1% triacontanol soluble liquid (produced by Zhejiang Dapeng Pharmaceutical Co., Ltd.) was used as a control agent, and water was used as a blank control. Then, the different formulations were diluted with water to obtain test agents. Then, mangoes of the variety Taigong No. 1 were used as test objects. During the test, 5 mango trees were applied with the same test agent, and each tree was applied with only one test agent. Before the application, each tree was marked with 3 flower clusters in the east, south, west, north, and center directions, and the diameter of the young fruits on the flower clusters was 0.8-1 cm. The total amount of young fruits on the flower clusters was kept consistent. Then, the marked flower clusters were immersed in the test agent to soak the young fruits with the test agent. The test period was 2 times of application, and the interval between the two applications was 7 days. The soaking time of each flower cluster in the test agent was the same during each application. The longitudinal and transverse diameters of the fruits were investigated on the day before the first application, and then the longitudinal and transverse diameters of the fruits were investigated on the 7th day after the first application, and the second application was carried out at the same time. The longitudinal and transverse diameters of the fruits were investigated on the 7th day after the second application. Finally, the average increase of the longitudinal and transverse diameters of the fruits on the 7th day after the first application and the average increase of the longitudinal and transverse diameters of the fruits on the 7th day after the second application were calculated.

[0281] The number of each test agent, the concentration of the active ingredients (2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and triacontanol) in each test agent, and the increase of the longitudinal and transverse diameters of the fruits on the 7th day after the first application and the increase of the longitudinal and transverse diameters of the fruits on the 7th day after the second application after using each test agent are shown in Table 36.

[0282] Table 36 Number of each test agent, concentration of active ingredients in each test agent, and increase of longitudinal and transverse diameters of mango young fruits of each test agent

[0283]

[0284] As can be seen from Table 36, compared with water, the liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Examples 7-8 can promote the growth of the longitudinal diameter and the transverse diameter of the mango fruit after the fruit is soaked, and the promoting effect is obviously improved as the concentration of the active ingredient increases. In addition, when the concentration of the active ingredient is the same, compared with the control agent, the growth amount of the longitudinal diameter and the transverse diameter of the mango fruit is obviously larger on the 7th day after the second application of the liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Examples 7-8, which indicates that the liquid formulations containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine of Examples 7-8 have a better promoting effect on the growth of the mango fruit.

Claims

1. A liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine, characterized in that, The liquid preparation mainly consists of active ingredients, emulsifiers, solvents and co-solvents; the active ingredients consist of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and a complexing agent; the complexing agent is gibberellic acid GA3 or gibberellic acid GA4+7; the co-solvent is dimethyl sulfoxide or N,N-dimethylformamide; the mass fraction of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine in the liquid preparation is not more than 10%; the mass fraction of the complexing agent in the liquid preparation is not more than 30%; the liquid preparation comprises a stabilizer, which is formic acid and / or lactic acid; and the liquid preparation is a clear and transparent liquid.

2. A liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine according to claim 1, characterized in that, The complexing agent is gibberellic acid GA3, and the mass fractions of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and gibberellic acid GA3 in the liquid preparation are independently not more than 0.9%; Or the complexing agent is gibberellic acid GA4+7, and the mass fractions of 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine and gibberellic acid GA4+7 in the liquid preparation are independently not more than 1.8%.

3. A liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine according to claim 1, characterized in that, The complexing agent is gibberellic acid GA3, and the mass fraction of the stabilizer in the liquid preparation is 0.5-2%; Or the complexing agent is gibberellic acid GA4+7, and the mass fraction of the stabilizer in the liquid preparation is 10-20%.

4. A liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine according to claim 1 or 2, characterized in that, The complexing agent is gibberellic acid GA3, and the emulsifier in the liquid preparation is octylphenol polyoxyethylene ether and / or fatty alcohol polyoxyethylene ether; and the mass fraction of the emulsifier in the liquid preparation is 1-4%; Or the complexing agent is gibberellic acid GA4+7, and the emulsifier in the liquid preparation is octylphenol polyoxyethylene ether and / or fatty alcohol polyoxyethylene ether; and the mass fraction of the emulsifier in the liquid preparation is 2-4%.

5. A liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine according to claim 1 or 2, characterized in that, The complexing agent is gibberellic acid GA3, and the co-solvent in the liquid preparation is dimethyl sulfoxide; and the mass fraction of the co-solvent in the liquid preparation is 15-25%; Or the complexing agent is gibberellic acid GA4+7, and the co-solvent in the liquid preparation is N,N-dimethylformamide; and the mass fraction of the co-solvent in the liquid preparation is 30-40%.

6. A liquid formulation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine according to claim 1 or 2, characterized in that, The complexing agent is gibberellic acid GA3, and the solvent in the liquid preparation is an alcohol solvent, which is ethylene glycol and / or propylene glycol; Or the complexing agent is gibberellic acid GA4+7, and the solvent in the liquid preparation is an alcohol solvent, which is ethylene glycol and / or propylene glycol.

7. A process for the preparation of a liquid formulation containing 2-fluoro-N-(3- methoxyphenyl)-7H-purin-6-amine according to any one of claims 1 to 6, characterized in that, The method comprises the following steps: uniformly mixing the formula amount of each component to obtain a liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine.

8. Use of the liquid preparation containing 2-fluoro-N-(3-methoxyphenyl)-7H-purin-6-amine as claimed in any one of claims 1-6 as a plant growth regulator.

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