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Macrolide benzoate compound and application thereof

A technology of benzoate compounds and macrolides, which is applied in the field of macrolide benzoate compounds and preparations, can solve the problems of poor insecticidal efficacy and drug efficacy stability, and achieve a solution Pollution and environmental protection cost issues, improvement of food safety, effect of less dosage

Inactive Publication Date: 2015-04-08
河北艾林化工科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For this reason, the technical problem to be solved by the present invention is the poor problem of insecticidal efficacy and drug efficacy stability of the avermectin B2 component isolated in the prior art, and then provides a kind of based on abamectin B2a Component macrolide benzoate compound, preparation method and application for the preparation of pesticides

Method used

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  • Macrolide benzoate compound and application thereof
  • Macrolide benzoate compound and application thereof
  • Macrolide benzoate compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The preparation of embodiment 1 intermediate

[0041] The present embodiment adopts the following steps to synthesize the intermediate compound shown in formula (II):

[0042]

[0043] (1) 5-position hydroxyl protection: take the abamectin B2a80kg shown in formula (a) and dissolve in 550kg dichloromethane solvent, and the feed liquid is cooled to-15 ℃, drop 18kg chloroformic acid alkenes while cooling The 45kg dichloromethane solution of propyl ester and 14kg tetramethylethylenediamine is reacted; After the reaction is terminated, the pH value of the system is adjusted to neutrality, and dichloromethane is added for extraction, and 5 shown in formula (b) is obtained after precipitation. Position protected abamectin B2a compound;

[0044](2) Oxidation of hydroxyl group at the 4″ position: Dissolve the compound (b) obtained in step (1) in 15kg of isopropyl acetate solvent, then add dimethyl sulfoxide and triethylamine to mix, and cool to -20 ℃, then add 21kg phenyl p...

Embodiment 2

[0047] Embodiment 2 compound preparation

[0048] The present embodiment adopts the following steps to synthesize the compound shown in formula (I):

[0049]

[0050] Get the intermediate shown in the formula (II) prepared in Example 1, and add the amount of benzoic acid calculated according to the molar ratio of 1:1.05, and carry out the salt-forming reaction under the conditions of controlling temperature 75°C and pressure-0.09Mpa to obtain A compound represented by formula (I).

[0051] Gained compound is carried out HPLC-MS detection, and its detection result sees figure 1 and figure 2 , it can be seen that the structural formula of the product is correct.

experiment example 1

[0053] Experimental example 1 2% emamectin B2 benzoate control of sweet potato stem nematode

[0054] 1 Experiment purpose

[0055] This experiment studies the field effect of 2% test product EC in controlling D. Appropriate application period, dosage, duration and method of application.

[0056] 2 Experimental conditions

[0057] 2.1 Selection of experimental objects, crops and varieties

[0058] Experimental object: sweet potato stem nematode; experimental crop: sweet potato.

[0059] 2.2 Environmental or Facility Cultivation Conditions

[0060] The experiment is located in Xushui County, Baoding City, Hebei Province. The sweet potato field covers an area of ​​about 1,000 mu. It has complete hydropower facilities, high soil fertility, good cultivation and management conditions, and is planted all year round.

[0061] 3 Experimental Design and Arrangement

[0062] 3.1 Pharmacy

[0063] 3.1.1 Experimental agents

[0064] Containing 2% emulsifiable concentrate of the co...

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Abstract

The invention belongs to the field of pesticides and in particular relates to a macrolide benzoate compound, a preparation method and application thereof. The compound has a structure which is shown in a formula (I). The invention also discloses an intermediate for preparing the compound, a preparation method of the compound and application of the compound to preparation of an agricultural insecticide. The compound is characterized by taking abamectin B2a as an initial raw material and preparing a stable compound in the form of methylamino phenyl formate. When the content of effective components and the dosage form are as the same as that of a preparation under the condition that the stable structure of the compound is ensured, the pesticide effect is 5-10 times that of the original compound; the compound discovered at present has a maximum activity on root-knot nematode; the toxicity of the compound is much lower than the existing pesticide for preventing and treating knot nematodes; the compound is of great help to improve the food safety; meanwhile, the environmental compatibility is obviously superior to other chemical synthesis pesticides; the consumption of the compound is extremely low.

Description

technical field [0001] The invention belongs to the field of pesticides, and in particular relates to a macrolide benzoate compound, a preparation method and an application. Background technique [0002] my country is a large agricultural country, with about 400 million hectares of crop diseases, insect pests and weeds occurring all year round, and 800,000 tons of pesticides need to be produced and used every year. Pesticides have become an indispensable element in agricultural production. However, the long-term irrational use of chemical pesticides has also brought many disadvantages such as environmental pollution, direct poisoning of non-target organisms, and negative effects such as plant resistance. Therefore, research on new pesticides with good environmental compatibility, safety, low residue and economy will become the development trend in the future. [0003] Abamectin is a new type of antibiotic pesticide developed in my country in the past 20 years. It is a micro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/08C07H1/00A01N43/90A01P5/00A01P7/04
Inventor 孟水强
Owner 河北艾林化工科技有限公司
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