Synthesis method of nitrogenous medicine intermediate indole derivative

Abstract

The invention relates to a synthesis method of an indole derivative shown by a nitrogenous medicine intermediate (III). The method comprises the following steps of in a solvent and in the insert gas atmosphere, under the existence of catalysts, nitrogenous ligands and acid promoters, a compound shown by a formula (I) and a compound shown by a formula (II) take a reaction; after the reaction is completed, post treatment is performed, so that a compound shown by the formula (III) is obtained. The formulas (I), (II) and (III) are shown as the accompanying drawing, wherein the R1 is selected from H or halogen; the R2 is selected from H, C1-C6 alkyls, C1-C6 alkoxy or halogen; or R2 and the substituted phenyl jointly form naphthyl. The method has the advantages that through the comprehensive selection and cooperation of the proper substrates, catalysts, nitrogenous ligands, acid promoters, solvents and the like, the range of the substrates is expanded; the aryl-substituted indol compound can be obtained at a good yield, so that the good application prospects and study values are realized in the field of organic chemical synthesis. The fire-new method is provided for the synthesis of the compounds of the kind.

Description

technical field [0001] The invention relates to a method for synthesizing a heterocyclic condensed compound, in particular to a method for synthesizing an indole derivative, a nitrogen-containing drug intermediate, and belongs to the technical field of organic chemical synthesis. Background technique [0002] In the field of organic chemical synthesis technology and medicinal chemistry, indole compounds, as a nitrogen-containing fused ring compound, often exist as important parent building blocks, intermediates and / or active units in the field of medicinal chemical intermediate synthesis technology , which also plays an important role and status in functional materials. [0003] For example, in the following drugs, the indole ring is its parent structure: [0004] [0005] It is precisely because of the important uses and application prospects of indole compounds that people have conducted a lot of research on their synthesis methods, mainly C-C coupling reactions, or co...

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Problems solved by technology

[0016] As mentioned above, although multiple methods for synthesizing indole compounds have been disclosed in the prior art, there are still some defects in these methods, such as low product yield, too expensive catalyst or too large amount of catalyst, too cumbersome reaction, and the substrate is still Need to expand etc.

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