Preparation method of N-(2-pyridyl/pyrimidyl)indole derivative

Abstract

The invention discloses a preparation method of an N-(2-pyridyl / pyrimidyl)indole derivative. The preparation method of the N-(2-pyridyl / pyrimidyl)indole derivative comprises the following steps: mixing a 2-substituted phenylaminopyridine / pyrimidine derivative, an alkenyl azide compound, a catalyst, an oxidizing agent, alkali and an organic solvent uniformly, heating to 60 to 80 DEG C under nitrogen or air, performing a cyclization reaction for 18 to 24 hours, cooling to room temperature after the reaction, and performing concentration and column chromatographic purification to obtain the N-(2-pyridyl / pyrimidyl)indole derivative. By the preparation method, the N-(2-pyridyl / pyrimidyl)indole derivative with various substituent groups which cannot be synthesized according to other methods canbe synthesized; furthermore, the used raw materials are easily available, the yield is high, the reaction condition is mild, the reaction time is short, the substrate range is wide, the reaction specificity is high and aftertreatment is simple, convenient and green.

Description

technical field

[0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a preparation method of N-(2-pyridine / pyrimidinyl) indole derivatives. Background technique

[0002] N-(2-pyridine / pyrimidinyl)indole derivatives are a class of widely used intermediates in organic synthesis, and have important application values ​​in natural products, pharmaceutical production, and organic synthesis. Therefore, the study of new preparation methods for multi-substituted indoles has important application value and has attracted the attention of researchers in related fields.

[0003] Traditional methods for the synthesis of N-(2-pyridine / pyrimidinyl) indole derivatives include Fischer indole synthesis; Larock indole synthesis; transition metal-catalyzed 2-multisubstituted phenylaminopyridine derivatives with 1,2-disubstituted Hydrocarbon cyclization reactions, etc. The above method generally has the following problems: 1) poor reaction regi...

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