Method for synthesizing alpha-benzyl benzofuran compound

Abstract

The invention discloses a method for synthesizing an alpha-benzyl benzofuran compound, which comprises the following step of: reacting a benzofuran compound and an aryl ethylene compound serving as raw materials in a solvent in the presence of a catalyst and organic alkali in an inert gas atmosphere to obtain the alpha-benzyl benzofuran compound. Compared with the existing method, the method disclosed by the invention has the advantages that the direct use of an air-sensitive zero-valent nickel complex as a catalyst is avoided, and the applicability of the substrate is obviously expanded; provided is a novel method for producing the alpha-benzyl benzofuran compound by a hydroheteroarylation reaction of an arylethene compound and a benzofuran compound, said method being achieved by an air-stable divalent nickel-based catalyst.

Description

technical field

[0001] The invention belongs to the technical field of organic synthesis preparation, and in particular relates to a method for synthesizing α-benzylbenzofuran compounds. Background technique

[0002] Benzofuran and its derivatives not only widely exist in natural products and bioactive molecules, but also are general structural units for the construction of drug molecules (see Horton, D. A.; Bourne, G. T.; Smythe, M. L. Chem. Rev. 2003, 103 , 893). In benzofuran derivatives, the alkylation of the β-position on the benzofuran backbone can now be catalyzed by Lewis or Bronsted acids (see Rueping, M.; Nachtsheim, B. J. Beilstein J. Org. Chem. 2010, 6 , 6). However, there are still relatively few methods for the alkylation of the α-position on the benzofuran skeleton, and there are obvious limitations. For example, Yoshiaki's research group used an air-sensitive zero-valent nickel catalyst to realize the hydroheteroarylation reaction of styrene and ben...

Images