A kind of preparation method of 1-aminoindole derivative

A technology of aminoindole derivatives and derivatives, which is applied in the field of preparation of 1-aminoindole derivatives, can solve the problems of unfriendly environment, pre-preparation of substrates, harsh reaction conditions, etc., and achieve strong reaction specificity, Post-processing green, easy post-processing effect
CN107098847BActive Publication Date: 2019-07-09HUAQIAO UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HUAQIAO UNIVERSITY
Publication Date
2019-07-09

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Abstract

The invention discloses a preparation method of a 1-amino indole derivative. The method comprises the steps of mixing a phenylhydrazine hydrochloride derivative, a diazo compound, an aldehyde or ketone compound, a catalyst, alkali and an organic solvent evenly; and carrying out condensation reaction in air or nitrogen at 80-100 DEG C for 2-12h to obtain the 1-amino indole derivative. The 1-amino indole derivative which cannot be synthesized by other others can be synthesized, and the used raw materials are available, high in yield, mild in reaction condition, wide in substrate range, high in reaction specificity, and simple and green in aftertreatment.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a preparation method of 1-aminoindole derivatives. Background technique

[0002] 1-Aminoindole derivatives are a class of organic synthesis intermediates with a wide range of uses, and have important application values ​​in natural products, biomedicine, and organic synthesis. Therefore, the research on the new synthesis method of 1-aminoindole has important application value, and has attracted the attention of scientific researchers in related fields.

[0003] The traditional methods for synthesizing 1-aminoindole derivatives include palladium-catalyzed intramolecular condensation reaction of o-chloroaryl acetaldehyde N-N dimethylhydrazone, and palladium-catalyzed intermolecular condensation reaction of o-chlorophenylacetylene and N-N disubstituted hydrazine. However, there are many problems in these methods, such as: 1) the use of halides is not environme...

Claims

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