Synthesis method of 2, 5-disubstituted thiophene compound

Abstract

The invention relates to a preparation method of 2, 5-disubstituted thiophene compound I and the usage of the 2, 5-disubstituted thiophene compound in preparation of compound V. The preparation method is used for synthesizing the compound I by a 'one-pot' method through compound II and compound III under the condition that sulfur reagent exists. Compared with the prior art, the invention has the advantages of being easy in material obtaining, mild in reaction condition, simple and convenient in operation, high in yield, suitable for industrialized production and the like.

Description

technical field The invention belongs to the field of medicinal chemistry, and more specifically, the invention relates to a preparation method of a 2,5-disubstituted thiophene compound represented by general formula I and a method for preparing a compound represented by general formula V using it. Background technique There are two main methods of compound shown in the existing synthetic formula I: 1) Friedel-Crafts reaction The reaction makes 2-substituted thiophene and acid halide or anhydride in anhydrous AlCl 3 Under the catalysis, generate the compound shown in general formula I. For example, U.S. Patent Application No. 20050233988A1 discloses 2-phenylthiophene and benzoyl chloride in AlCl 3 A method for the formation of 2-phenyl-5-benzoylthiophene in the presence. The disadvantages of the above methods include: (1) 2-aryl substituted thiophene is not easy to get, and it needs to be catalyzed by expensive palladium reagent through Suzuki coupling reaction; (...

AI Technical Summary

Problems solved by technology

The disadvantages of the above methods include: (1) 2-aryl substituted thiophene is not easy to get, and it needs to be catalyzed by expensive palladium reagent through Suzuki coupling reaction; (2) AlCl 3 It is flammable when it meets water, and the aluminum salt formed