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Pyrazol derivative and preparation method and application thereof

A technology of pyrazole derivatives and C1-C20, which is applied in the field of acaricide and agricultural insecticide, and can solve the problems of undisclosed pyrazole derivatives, etc.

Active Publication Date: 2018-09-25
ZHEJIANG RES INST OF CHEM IND CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The prior art does not disclose the pyrazole derivatives described in the present application

Method used

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  • Pyrazol derivative and preparation method and application thereof
  • Pyrazol derivative and preparation method and application thereof
  • Pyrazol derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0203] Embodiment 1, intermediate preparation

[0204] (1) Synthesis of intermediate 1-ethyl-3-methyl-5-pyrazole carboxylic acid ethyl ester

[0205]

[0206] 154.1g (1mol) intermediate A is added in the flask of 1000ml, add 500ml acetonitrile and 138g potassium carbonate, then add 1mol diethyl sulfate, the system is stirred and heated to reflux reaction, plate chromatography traces about 3hr reaction is completed, system filtration, The mother liquor was evaporated to dryness with a rotary evaporator, and the residue was distilled under reduced pressure to obtain 140 g of Intermediate B with a yield of 77.0%.

[0207] (2) Synthesis of intermediate 1-ethyl-3-methyl-4-chloro-5-pyrazole ethyl carboxylate

[0208]

[0209] Add 18.2g (0.1mol) of intermediate B to a 100ml flask, add 50ml of dichloroethane and 138g of potassium carbonate, then add 0.11mol of sulfonyl chloride, the system is stirred and heated to reflux, and the reaction is completed by plate chromatography trac...

Embodiment 2

[0249] Embodiment 2, target compound preparation

[0250] (1) Target compound 226

[0251]

[0252] Add 0.31g (0.001mol) of intermediate TA-1 and 0.12g (0.0011mol) of intermediate F-1, 0.15g of sodium carbonate and catalytic amount of sodium iodide into 25ml of acetonitrile, then heat to reflux for 7hrs, and follow the plate chromatography After the reaction was completed, the reaction system was cooled to room temperature, the solid was removed by filtration, acetonitrile was distilled off, and the residue was purified by column chromatography to obtain 0.32 g of the product with a yield of 84%.

[0253] (2) Target compound 251

[0254]

[0255] Add 31g (0.1mol) of intermediate TA-1 and 13g (0.11mol) of intermediate F-2, 15 sodium carbonate and a catalytic amount of sodium iodide into 250ml of acetonitrile, then heat and reflux for 10 hours, and follow the completion of the reaction by plate chromatography , the reaction system was cooled to room temperature, the soli...

Embodiment 3、30

[0285] Embodiment 3, 30% suspending agent

[0286]

[0287]

[0288] Compound 251 and other components were thoroughly mixed to obtain a 30% suspension concentrate. Dilution with water to give a 30% suspension concentrate can give any desired concentration of dilution.

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PUM

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Abstract

The invention discloses a pyrazol derivative as shown in general formula stru-1, wherein various substituents are defined in the specification. The pyrazol derivative is applicable to pest control.

Description

technical field [0001] The invention belongs to the field of agricultural insecticide and acaricide, and specifically relates to a class of pyrazole derivatives. Background technique [0002] Due to the long-term use of the existing pesticides, the pests and diseases have developed resistance, which has significantly increased the use of pesticides and caused serious damage to the environment. Therefore, it is required to continuously discover new efficient pesticides with new mechanisms of action, such as new pesticides with higher activity for killing insects, bacteria or acaricides. For example, among the existing acaricide pesticide varieties, most pesticides can only control mite eggs It is one of the three stages of mites, nymphs, and adults. It will be of great significance to research and develop a new acaricide that has control effects on all three stages of mites. [0003] PCT patent application WO01 / 68589 discloses heterocyclic acrylonitrile ether compounds, and ...

Claims

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Application Information

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IPC IPC(8): C07D231/12C07D231/16A01N47/06A01N43/56A01P5/00A01P7/02A01P7/04
CPCA01N43/56A01N47/06C07D231/12C07D405/12C07D401/12
Inventor 许天明袁静钟良坤郁季平彭伟立胡冬松魏优昌孔小林郑志文邢家华
Owner ZHEJIANG RES INST OF CHEM IND CO LTD
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