The synthetic method of substituted indole-2-carboxylic acid

A synthesis method and indole technology, which is applied in the synthesis of important intermediates of medicine and pesticides, and in the field of synthesis of substituted indole-2-carboxylic acid, can solve the problem of waste gas, waste water, waste, unfavorable industrial application, complex process, etc. problems, to achieve environmental friendliness, significant social and economic benefits, and easy access to raw materials
CN104402795BInactive Publication Date: 2017-10-13CHINA AGRI UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CHINA AGRI UNIV
Publication Date
2017-10-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthetic method of substituted indol-2-formic acid. Substituted phenylhydrazine hydrochloride or phenylhydrazine is used as a raw material, hydrazone is formed through ethyl pyruvate, then substituted indol-2-ethyl formate is obtained through a Fischer indol synthetic reaction, and the substituted indol-2-formic acid is obtained after hydrolysis. The product purity is greater than 97%, and the reaction yield is 64%. The synthetic method disclosed by the invention has the characteristics of being free of severe conditions, simple to operate and environment-friendly, and has certain economic benefit. According to the synthetic method of the indol-2-formic acid, the raw materials are easily obtained, the operation is simple and convenient, three wastes are few, and the yield is high.
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Description

technical field

[0001] The invention relates to the synthesis of an important intermediate of medicine and pesticide, especially the synthesis method of substituted indole-2-carboxylic acid. It belongs to the field of organic synthesis. Background technique

[0002] Substituting indole-2-carboxylic acid medicine, an important intermediate of pesticides, with the in-depth development of pyrimidine pesticides and medicines, indole-2-carboxylic acid has been more and more widely used as an intermediate. Therefore, the research and development of substituted indole-2-carboxylic acids is of great significance.

[0003] At present, there are several methods for the synthesis of substituted indole-2-carboxylic acids:

[0004] One: Hemetersberger reaction, condensation of substituted benzaldehyde and ethyl azidoacetate, and then ring-closing under catalytic heating conditions to obtain substituted indole-2-carboxylate, and then hydrolyzed to obtain acid. This type of method has a ...

Claims

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