A method for directly constructing indolo ring compounds

A technology for cyclic compounds and indole, which is applied in the field of direct synthesis of indole ring compounds through aryl side chain C-H bond activation, can solve problems such as difficult to avoid metal residues in synthetic drugs, difficult to control, high reaction selectivity of equipment, etc., to achieve production The effect of high efficiency, mild conditions and simple operation
CN110283179BActive Publication Date: 2021-10-01UNIV OF SCI & TECH OF CHINA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
UNIV OF SCI & TECH OF CHINA
Publication Date
2021-10-01

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Abstract

The invention discloses a method for directly constructing indolo ring compounds, which is characterized in that 2-[(2-iodobenzyl) oxo]benzonitrile derivatives are used as substrates, and catalyst copper salt and alkali, 2 ‑[(2‑iodobenzyl)oxo]benzonitrile derivatives in a molar ratio of 0.02~0.2:2~4:1, react in a solvent at 90°C for 8‑20h, and use petroleum ether / dichloromethane / Ethyl acetate was mixed at a volume ratio of 20 to 5:2:1 as an eluent, and separated through a silica gel column to obtain the target product. The method of the invention has the advantages of simple operation, mild conditions and high yield, and is a green and novel synthetic method.
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Description

technical field

[0001] The invention belongs to the technical field of methods for directly constructing indolo ring compounds, and in particular relates to a method for directly synthesizing indolo ring compounds by activating an aryl side chain C-H bond. Background technique

[0002] Indole tetracyclic structural units widely exist in organic intermediates, pharmaceutical compounds and organisms, so the direct construction of indolocyclic compounds has a wide range of applications in the fields of materials chemistry and medicinal chemistry. However, the existing methods for the synthesis of indolo ring compounds basically require the use of transition metals as catalysts. However, the high oxidant and metal residues of transition metal complexes limit their large-scale application in industry and pharmaceutical industry. And most of the synthetic methods of indolocyclic compounds are to use indole and derivatives thereof as raw materials to synthesize indolocyclic compou...

Claims

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