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Novel amide-esbiothrin-type chemical modification substance and preparation method and application thereof

A technology of chemical modification of amidothrin and its application in the field of new type of chemical modification of amidothrin and its preparation, which can solve problems such as threats to human and animal health, interference with biological functions, and adverse effects on children's health, and achieve drug resistance Good insecticidal effect, excellent transformation potential

Inactive Publication Date: 2019-04-19
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, more and more studies have found that pyrethroids can interfere with the normal function of organisms and pose a considerable threat to human and animal health
Studies have shown that long-term exposure to pyrethroid-containing environments will have adverse effects on the health of humans, especially children
Moreover, with the long-term single use of some traditional pyrethroid insecticides in large quantities, pests such as mosquitoes and flies have obvious resistance to pesticides, so a new type of insecticide compound with high efficiency and low toxicity is needed

Method used

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  • Novel amide-esbiothrin-type chemical modification substance and preparation method and application thereof
  • Novel amide-esbiothrin-type chemical modification substance and preparation method and application thereof
  • Novel amide-esbiothrin-type chemical modification substance and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0037] The preparation of embodiment 1 novel chrysanthemum chemical modification (DCA-CONH-01)

[0038] 1. The preparation of a novel chrysanthemum chemical modification (DCA-CONH-01), comprising the following steps:

[0039] (1) First weigh 200mg (0.671mmol) of dibromochrysanthemic acid in a 50mL round-bottomed flask, under the condition of nitrogen protection, measure 15mL ultra-dry anhydrous dichloromethane in the flask with a syringe and stir to make After it is completely dissolved, add three times the amount of oxalyl chloride 0.171mL (2.014mmol), stir for about 30min, then add 0.1mL of anhydrous grade N,N-dimethylformamide (DMF) with a 1mL syringe, The reaction will produce a large number of bubbles, and then react at room temperature for 1h;

[0040] (2) The reaction-activated product in the round-bottomed flask after the reaction for 1h is rotary-evaporated and dried in a vacuum rotary evaporator, and during the operation, the external air is reduced as far as possib...

Embodiment 2

[0046] The preparation of embodiment 2 novel chrysanthemum chemical modifications (DCA-CONH-02)

[0047] 1. The preparation of novel chrysanthemum amide chemical modification (DCA-CONH-02), comprising the following steps:

[0048] (1) First weigh 200mg (0.671mmol) of dibromochrysanthemic acid in a 50mL round-bottomed flask, under the condition of nitrogen protection, measure 15mL ultra-dry anhydrous dichloromethane in the flask with a syringe and stir to make After it is completely dissolved, add three times the amount of oxalyl chloride 0.171mL (2.014mmol), stir for about 30min, then add 0.1mL of anhydrous grade N,N-dimethylformamide (DMF) with a 1mL syringe, The reaction will produce a large number of bubbles, and then react at room temperature for 1h;

[0049] (2) The reaction-activated product in the round-bottomed flask after the reaction for 1h is rotary-evaporated and dried in a vacuum rotary evaporator, and during the operation, the external air is reduced as far as p...

Embodiment 3

[0055] The preparation of embodiment 3 novel chrysanthemum chemical modifications (DCA-CONH-03)

[0056] 1. The preparation of a novel chrysanthemum chemical modification (DCA-CONH-03), comprising the following steps:

[0057] (1) First weigh 200mg (0.671mmol) of dibromochrysanthemic acid in a 50mL round-bottomed flask, under the condition of nitrogen protection, measure 15mL ultra-dry anhydrous dichloromethane in the flask with a syringe and stir to make After it is completely dissolved, add three times the amount of oxalyl chloride 0.171mL (2.014mmol), stir for about 30min, then add 0.1mL of anhydrous grade N,N-dimethylformamide (DMF) with a 1mL syringe, The reaction will produce a large number of bubbles, and then react at room temperature for 1h;

[0058] (2) The reaction-activated product in the round-bottomed flask after the reaction for 1h is rotary-evaporated and dried in a vacuum rotary evaporator, and during the operation, the external air is reduced as far as possi...

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Abstract

The invention discloses a novel amide-esbiothrin-type chemical modification substance and a preparation method and application thereof. The structural formula of the novel amide-esbiothrin-type chemical modification substance is shown in the description, wherein R is a monosubstituted or polysubstituted aromatic-ring-type group. According to the chemical modification substance, two end chlorine atoms and an ester group on transfluthrin are mainly modified and transformed, the two end chlorine atoms are replaced by two bromine atoms, the ester group is replaced by the acylamino structure, ring-type substitution is most aromatic-ring substitution, and a series of novel amide-esbiothrin-type derivative structures containing dibromo-substituted and amide group structures are formed. The novelamide-esbiothrin-type derivatives have a certain insect-killing and mosquito-killing effect on larvae and adult mosquitos, the metabolism stability can also be improved, the environment toxicity is lowered, the serious problem of obvious drug resistance of existing pyrethroids-type insecticide can be effectively solved, and the chemical modification substance has excellent transformation potentialand is wide in application prospect.

Description

technical field [0001] The invention belongs to the technical field of pesticides for structure modification of medicine small molecules. More specifically, it relates to a novel amidothrin chemical modification and its preparation method and application. Background technique [0002] Blood-sucking female adult mosquitoes are intermediate hosts for pathogens that transmit dengue fever, malaria, yellow fever, filariasis, and Japanese encephalitis. The hot temperature and humid humidity in summer provide suitable conditions for the breeding and infestation of mosquitoes. The whole summer and even part of autumn is the time for mosquitoes to reproduce and appear. The habits of mosquitoes have brought great harm and influence to people's daily life, especially for Aedes albopictus, also known as the Asian tiger stripe, which has Strong vitality, cold resistance and vitality, and fast reproduction and transmission speed, it is a common mosquito species in Southeast Asia and Chi...

Claims

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Application Information

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IPC IPC(8): C07C231/02C07C233/58C07C233/59C07C233/60C07C253/30C07C255/58A01N53/12A01P7/04C07C51/60C07C61/40
CPCA01N53/00C07C51/60C07C61/40C07C231/02C07C233/58C07C233/59C07C233/60C07C253/30C07C255/58C07C2601/02
Inventor 赵肃清张炳杰冯冬燕方颖林吴可凌华英谭绮婷陈燕婷杨洋赵佳伟马焯霖洪为谦
Owner GUANGDONG UNIV OF TECH
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