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Preparation method of quintuple nitrogen heterocyclic pesticide

A nitrogen heterocycle and pesticide technology, which is applied in the field of preparation of five-membered nitrogen-containing heterocycle pesticides, can solve the limitations of promotion and application, do not provide derivatives of benzimidazole ring, triazole ring and thiadiazole ring, and cannot Agricultural production services, etc.

Inactive Publication Date: 2013-03-27
杨春文
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Problems solved by technology

[0010] The present invention provides a preparation method of a five-membered nitrogen-containing heterocyclic pesticide, which aims to solve the problem of biological activity of derivatives containing benzimidazole rings, triazole rings and thiadiazole rings that are not provided in the prior art. The characteristics are undeveloped, which greatly restricts the promotion and application of pesticides containing benzimidazole rings, triazole rings and thiadiazole ring derivatives, and cannot better serve agricultural production.

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  • Preparation method of quintuple nitrogen heterocyclic pesticide
  • Preparation method of quintuple nitrogen heterocyclic pesticide
  • Preparation method of quintuple nitrogen heterocyclic pesticide

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preparation example Construction

[0026] The preparation method comprises the following steps:

[0027] In step S101, using o-phenylenediamine as a raw material, the corresponding intermediate 2-substituted benzimidazole-1-carboxylic acid is synthesized by cyclization and N-alkylation reaction;

[0028] In step S102, the key intermediate 1-amino-2-(2-substituted benzimidazole-1-alkyl)-5-mercaptotriazole is synthesized by reacting the intermediate with 1,4-dithiosemicarbazide;

[0029] In step S103, the key intermediates synthesized are respectively combined with CS 2 Cyclization followed by S-alkylation and re-acylation with BrCN to obtain heterocyclic derivatives of the target compound benzimidazole ring and triazole ring;

[0030] In step S104, the structure of the synthesized target compound is demonstrated through modern physical technology tests.

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Abstract

The invention discloses a preparation method of a quintuple nitrogen heterocyclic pesticide, which takes o-phenylenediamine as a raw material and comprises the following steps of: synthesizing a corresponding intermediate 2-substituted benzimidazole-1-carboxylic acid through cyclization and N-alkylation reaction; synthesizing a key intermediate 1-amino-2-(2-substituted benzimidazole-1-alkyl)-5-mercaptotriazole through a reaction between the intermediate and 1,4-dithiosemicarbazide; cyclizing the synthesized key intermediate with CS2 and conducting an S-alkylation reaction, and cyclizing the synthesized key intermediate with BrCN and conducting an acylation reaction to obtain a target compound heterocyclic derivative of a benzimidazole ring and a triazole ring; testing with the modern physical technology, and performing structure expression on the synthesized target compound; and performing the sterilization and weeding biological activity and toxicity test on the quintuple nitrogen heterocyclic pesticide to further screen out high-activity low-toxicity heterocyclic derivative containing the benzimidazole ring and the triazole ring to effectively guarantee the normal growth of crops.

Description

technical field [0001] The invention belongs to the field of a preparation method of a five-membered nitrogen-containing heterocyclic pesticide, and in particular relates to a preparation method of a five-membered nitrogen-containing heterocyclic pesticide. Background technique [0002] The current important trend in the development of pesticides is heterocyclic compounds, which have played a very important role in the development of pesticides. About 90% of the patents on pesticides in the world are heterocyclic compounds. The main reason is that they are in heterocyclic compounds. , the dosage of some ultra-efficient pesticides is very low, and the economic benefits are high. The large-scale use of such ultra-efficient pesticides not only reduces the cost, but more importantly, reduces the environmental damage to a small degree. In addition, most of the new pesticides of heterocyclic compounds have very low toxicity to warm-blooded animals, and also have low toxicity to bi...

Claims

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Application Information

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IPC IPC(8): C07D513/04A01P3/00A01P13/00
Inventor 杨春文
Owner 杨春文
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