abstract |
The invention belongs to the technical field of pharmaceutical chemical synthesis, and discloses a method for synthesizing 2,3-dihydrobenzofuran derivatives and indole derivatives substituted by fluorine-containing alkyl groups. The synthesis method is as follows: 2-allylphenol or 2-allylaniline compounds, iodine-substituted fluorine-containing reagents are used as raw materials, palladium is used as a catalyst, phosphine is used as a ligand, alkali is used as an additive, and an organic solvent is used as a solvent. Under a nitrogen atmosphere, stir and react at 60-100°C for 12-24 hours. After the reaction, cool to room temperature. The reaction solution is extracted with ethyl acetate, and the solvent is removed under reduced pressure to obtain a crude product, which is purified by column chromatography. The reaction is as follows: (I) shown. The present invention synthesizes fluorine-containing alkyl-substituted 2,3-dihydrobenzofuran derivatives and indole derivatives in one step, the synthesis method is simple and easy, the reaction conditions are mild, the adaptability to substrates is wide, and the product yield is high. It has good industrial application prospect. |