Method for synthesizing benzofuranol derivative by nickel-catalysis of phenethynyl phenol under microwave irradiation

Abstract

The invention discloses a method for synthesizing a benzofuranol derivative by nickel-catalysis of phenethynyl phenol under microwave irradiation; a catalytic amount of catalyst nickel chloride, ligand 1,10-phenanthroline(1,10-Phen), auxiliary catalyst potassium hydroxide, 2-phenylethynyl phenol and a derivative thereof and pure water are added into a reaction vessel, the reaction vessel is placedin a microwave reactor for reaction under certain temperature and power, after a certain period of time, vacuum concentration is performed, and a product is purified by column chromatography. The method for synthesizing the benzofuranol derivative is novel in raw materials, simple in operation and high in efficiency. Compared with the prior art, the reaction speed of the method is obviously faster than that under conventional heating, the reaction condition is mild, the operation is simple, the yield is high, and the method is safe and environmentally friendly.

Description

technical field [0001] The present invention relates to a method for preparing benzofuran derivatives. That is, using 2-phenylethynylphenol and its derivatives as raw materials, introducing microwave as an auxiliary synthesis method, and using transition metal nickel as the main catalyst, a method for efficiently catalyzing and rapidly preparing benzofuran derivatives. Background technique [0002] The structural units of 2-arylbenzofuran widely exist in natural products and artificially designed compounds. These compounds exhibit a variety of structural properties, and more importantly, they have a wide range of biological activities, diverse biological activities and great medicinal value. It has long been the focus of people's attention. Since the first 2-arylbenzofuran was reported in 1909, more than ten thousand kinds of arylbenzofuran have been discovered or synthesized. At the same time, some aryl benzofurans have also been used in the field of drug research. Most a...

AI Technical Summary

Problems solved by technology

Due to the limited amount and rare content of aryl benzofuran compounds extracted from natural products, it will be very important to artificially synthesize such compounds. With the continuous deepening of research on the synthesis of aryl benzofuran compounds, people have A large number of compounds have been synthesized for related structure-activity relationship research. However, the synthesis of such compounds still has a long route and harsh reaction conditions. Therefore, it is of great significance to explore and study the synthesis and properties of these compounds.

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