A kind of preparation method of N-(indole-n-formyl)-alpha-aminoamide derivative

Abstract

The invention discloses a preparation method of N-(indole-N-formyl)-α-aminoamide derivatives, which comprises the following steps: N-indole carboxylic acid compounds, aldehyde compounds, primary amine compounds and The four-component reaction of the isonitrile compound in the solvent; or the three-component reaction of the N-indole carboxylic acid compound, the cyclic imine compound and the isonitrile compound in the solvent. After the reaction is completed, the post-treatment obtains the N-(indole-N-formyl)-α-aminoamide derivative; the preparation method uses the indole compound as a potential component of the classic Ugi reaction, in mild The rapid connection of indole skeleton and α-aminoamide is realized under the conditions, the reaction is efficient, concise and fast, and the yield is high, which has far-reaching significance for organic synthesis and medicinal chemistry.

Description

technical field

[0001] The invention belongs to the field of organic synthesis, and in particular relates to a preparation method of N-(indole-N-formyl)-α-aminoamide derivatives. Background technique

[0002] The indole core is a dominant skeleton in natural products and medicinal chemistry, and the compounds containing the indole core are often important compounds with biological activity or medicinal value. The Ugi reaction is a classic multi-component reaction in organic synthesis. This reaction successfully synthesizes α-aminoamides from carboxylic acids, carbonyl compounds, primary amines and isonitriles in one pot. It is an unnatural amino acid derivative. Important methods of synthesis ((a) Ugi, I.; Meyr, R.; Fetzer, U.; Steinbrückner, C. Angew. Chem. 1959, 71, 386. (b) Ugi, I.; Steinbrückner, C. Angew. Chem. .1960,72,267.(c)Ugi,I.Angew.Chem.,Int.Edit.1962,1,8.), the classic Ugi reaction is as follows:

[0003]

[0004] The Ugi reaction has been developed for mor...

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