Pyrazol amidine derivative and application thereof in agriculture

A derivative, the technology of pyrazoamidine, which is applied in the field of pyrazoamidine derivatives and its application in agriculture, can solve the problems such as the reduction of control effect

Inactive Publication Date: 2010-06-30
GUANGDONG GEOLONG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are many insecticides and acaricides on the market, insects and mites will develop resistance to them after long-term use of insecticides and acaricides, which will reduce the control effect

Method used

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  • Pyrazol amidine derivative and application thereof in agriculture
  • Pyrazol amidine derivative and application thereof in agriculture
  • Pyrazol amidine derivative and application thereof in agriculture

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment one: the preparation of formula (XI) compound

[0023] Add 21.85g (0.05mol) of 1-(4-trifluoromethyl-2,6-dichlorophenyl)-3-cyano-4-trifluoromethylsulfinyl-5-aminopyrazole to the 14.82g (0.1mol) of triethyl orthoformate and 20ml of nitrobenzene in a 100ml reaction flask, then add 0.2g of p-toluenesulfonic acid monohydrate, heat the oil bath to about 150°C, condense and export the ethanol produced by the reaction, and wait The reaction was stopped when no ethanol flowed out, the unreacted triethyl orthoformate and the solvent were distilled off under reduced pressure, and the residue was separated by column chromatography to obtain 17.5 g of the target compound with a melting point of 70-72°C.

Embodiment 2

[0024] Embodiment two: the preparation of formula (IV) compound

[0025] Add 24.7g (0.05mol) of the compound of formula (XI) into a 100ml Erlenmeyer flask, add 50ml of toluene and stir to dissolve, then add 4.4g of morpholine, and stir for 30 minutes. After filtering and drying, 23g of the target compound was obtained, with a melting point of 150-154°C. The filtrate was concentrated in vacuo, filtered and dried to obtain 2g of the target compound.

Embodiment 3

[0026] Embodiment three: the preparation of formula (V) compound

[0027] Add 24.7g (0.05mol) of the compound of formula (XI) into a 100ml Erlenmeyer flask, add 50ml of toluene and stir to dissolve, then add 5.8g of 2,6-dimethylmorpholine, and stir for 30 minutes. After filtering and drying, 24g of the target compound was obtained, with a melting point of 108-112°C. The filtrate was concentrated in vacuo, filtered and dried to obtain 2g of the target compound.

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Abstract

The invention provides a pyrazol amidine derivative. The structural formula of the derivative is expressed by a formula (I), wherein X represents SO, SO2 or S; R1 represents CH2CH3 or CF3; and R2 represents NH2 or a compound of the formula (I) of groups (disclosed in the specification). The derivative comprises various isomers and salts thereof formed with various acids and has killing effect on pests and mites. The derivative or proper preparations compounded and prepared from the derivative with other bioactive compounds can be used for preventing and controlling pests and mites damaging agricultural, forestry and horticultural crops and agricultural and sideline products of the storage period.

Description

technical field [0001] The invention relates to a pyrazole amidine derivative and its application in agriculture. technical background [0002] Pests and mites harm almost all agricultural, forestry and horticultural crops worldwide, and also harm agricultural by-products during storage, and may cause devastating damage. Although there are many insecticides and acaricides on the market, insects and mites will develop resistance to them after long-term use of insecticides and acaricides, which will reduce the control effect. At the same time, with the emphasis on environmental protection and the implementation of sustainable development, there is an urgent need for pesticide creators to develop more efficient and low-toxic insecticides and acaricides. In other words, while emphasizing high activity, more attention should be paid to safety to ensure the safety of humans, the environment and non-target organisms. [0003] Multi-substituted pyrazole derivatives are a class of ...

Claims

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Application Information

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IPC IPC(8): C07D413/12C07D403/12C07D231/44A01N47/02A01P7/00
Inventor 高端阳符建立杨春燕梁仕权
Owner GUANGDONG GEOLONG BIOTECH
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