1,2-diarylindole, derivatives and synthesis method thereof

Abstract

The application relates to 1,2-diarylindole, derivatives and a synthesis method thereof, and a technical scheme for generating 1,2-diarylindole and derivatives without adding transition metal in organic solvent under oxygen atmosphere by taking iodine reagent and sulfoxide or sulphone reagent under the catalysis of secondary amine. The 1,2-diarylindole disclosed by the invention has the followingadvantages in comparison with the prior art: 1) the required reagent is stable in character, convenient to store, cheap and easy to obtain, and in favor of reducing the production cost; 2) the 1,2-diarylindole is in one-pot synthesis, the step economy advantage is extremely obvious, and synthesis is time-saving and labor-saving; 3) the region selectivity is excellent so as to manufacture a productwith a complex and variable structure, and the production of the isomer which is hard to separate is avoided; 4) the synthesis is free from using the transition metal, the pollution on the product bythe transition metal is eliminated; 5) the oxygen is taken as the oxidizing agent in the reaction, the water is used as the main byproduct, and is environmentally friendly; and 6) the whole reactionsystem is simple, the reaction equipment is less, and the experimental operation is simple and convenient.

Description

technical field [0001] The invention relates to 1,2-diarylindole, derivatives and a synthesis method thereof, belonging to the field of organic synthesis. Background technique [0002] 1,2-Diarylindole compounds are an important subclass of indole compounds, and many functional materials and bioactive molecules contain 1,2-diarylindole skeletons. So far, the synthetic methods of 1,2-diarylindole compounds have the following disadvantages: (I) required highly functionalized substrates, synthetic troubles, lively properties, inconvenient storage, and limited sources; (II) It needs to be carried out in multiple steps, and the step economy is poor, resulting in unnecessary waste of manpower and material resources, and poor operability; (III) when the aromatic rings of the target product have different groups, the regioselectivity is difficult to control, and often produce isomers that cannot be separated (IV) The pollution caused by the residual transition metals to the product...

AI Technical Summary

Problems solved by technology

So far, the synthetic methods of 1,2-diarylindole compounds have the following disadvantages: (I) required highly functionalized substrates, synthetic troubles, lively properties, inconvenient storage, and limited sources; (II) It needs to be carried out in multiple steps, and the step economy is poor, resulting in unnecessary waste of manpower and material resources, and poor operability; (III) when the aromatic rings of the target product have different groups, the regioselectivity is difficult to control, and often produce isomers that cannot be separated (IV) The pollution caused by residual transition metals to the product limits its application in drug synthesis, especially in the field of drug molecule synthesis for the human body

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