Method for synthesizing 2-indolone compound by catalytically oxidizing indole compound by iron

Abstract

The invention discloses a method for synthesizing a 2-indolone compound by catalytically oxidizing an indole compound by iron. The method comprises the step that in a water solution of an organic solvent, water or an organic solvent, hydrosilane is taken as an accelerant to prepare the 2-indolone compound (II) from an indole compound (I) under the action of an oxidizing agent and an iron catalyst. The method disclosed by the invention has the advantages of wide catalyst source, low cost and environment friendliness; the oxidizing agent is wide in source and low in cost and is environmentally friendly; the reaction conditions are mild, and selectivity and the yield are high; the substrate is wide in source and is stable; functional groups are good in compatibility and the substrate is wide in application range; and complex small molecules are compatible and can be well converted into ketone.

Description

technical field [0001] The invention relates to an iron-catalyzed method for synthesizing 2-indolinone compounds from oxidindole compounds, belonging to the technical field of 2-indolone compound synthesis. Background technique [0002] Indole, as a natural product and drug intermediate, has very common and wide applications. The skeleton of 2-indolinones is commonly found in natural products and pharmaceutical active molecules. Therefore, it is of great research significance and application value to develop a general, efficient, safe and economical method for synthesizing 2-indolinones. Indole compounds widely exist in natural products from a wide range of sources; it is of great significance to study them as raw materials to synthesize high value-added products. There are still some challenges in the current reaction of oxindole compounds, such as the need for expensive palladium catalysis; the need for ligands, which are expensive, toxic and difficult to recover; the nee...

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Problems solved by technology

[0003] Purpose of the invention: the purpose of the present invention is to solve the problem that the existing 2-indolinone compounds need noble metal catalysis, strong base, strong acid and / or expensive oxidant, resulting in low overall reaction yield, poor functional group compatibility and narrow application range , produce more waste discharge and environmental problems, provide a method for iron-catalyzed oxidation indole compounds to synthesize 2-indolinone compounds, the method only needs one-step reaction, does not require the participation of alkali and acid, and has a source of catalyst Wide range, low cost and environmental protection; cheap oxidant, green and environmental protection; wide and stable source of substrate; mild reaction conditions, good selectivity and high yield; good compatibility of substrate functional groups; complex small molecules can efficiently synthesize the corresponding 2 -Indolinones

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