The invention discloses a method for preparing a dihydropyrrole derivative and an intermediate
pyrrolidine thereof, and relates to the preparation of the
pyrrolidine and the dihydropyrrole derivative. Firstly, a diazocompound, amine, beta, gamma-unsaturated-alpha-keto ester with the mol ratio of 1.2 to 1.2 to 1 to 0.01 are weighed as raw materials,
metal Lewis acid is taken as a catalyst, the diazocompound is decomposed to form
metal carbine through a three-component tandem reaction under the
catalysis of the
metal Lewis acid,
ammonium ylide obtained by in-situ formation of the metal
carbine and the amine is captured by the beta, gamma-unsaturated-alpha-keto ester through the 1, 4-addition mode, then a corresponding intermediate
pyrrolidine derivative is obtained through intra-molecular condensation, finally the pyrrolidine derivative is mixed with an
organic solvent, then an
organic acid catalyst is added to form a
reaction system, and then the corresponding dihydropyrrole derivative is obtained through the water entrainment of a water segregator. The method has the advantages of high
atom economy, high efficiency, high yield and so on, and has safe and simple operation. The prepared pyrrolidine and the dihydropyrrole derivative are widely applied to the field of pharmaceutical and chemical industries.