Catalytic synthesis method of 2-substituted benzofuran compound

Abstract

The invention discloses a catalytic synthesis method of a 2-substituted benzofuran compound. The catalytic synthesis method includes the steps of dissolving 2-alkynyl substituted phenol in acetonitrile under normal temperature and normal pressure to obtain an acetonitrile solution of the 2-alkynyl substituted phenol, wherein the molar volume ratio of the 2-alkynyl substituted phenol to the acetonitrile is 1:1mmol / mL; adding cuprous chloride and cesium carbonate to the acetonitrile solution, wherein the molar ratio of each of the cuprous chloride and the cesium carbonate is 5% of that of the 2-alkynyl substituted phenol; stirring the solution at room temperature for 6 hours to generate the 2-substituted benzofuran compound after reaction. The catalytic synthesis method of the 2-substitutedbenzofuran compound has low cost and high yield; the cost of a catalyst required for preparing 1g of the 2-substituted benzofuran compound is reduced by two orders of magnitude as compared with that of existing synthesis methods in which iridium catalysts are used, and the yield is increased to 88.5 to 95.8%.

Description

technical field

[0001] The invention relates to a compound synthesis method, in particular to a catalytic synthesis method of 2-substituted benzofuran compounds. Background technique

[0002] 2-Substituted benzofuran compounds widely exist in natural products and pharmaceutical molecules, and have attracted much attention because of their good antibacterial, antioxidant, and antiviral activities. Using 2-alkynyl substituted phenols as raw materials, the synthesis of 2-substituted benzofuran compounds through intramolecular ring closure reaction is a relatively common preparation method, but expensive noble metal catalysts, equivalent Alkali or higher temperature, its preparation cost is higher, and product yield is moderate. As reported in the literature, the noble metal iridium catalyst can convert 2-(2-phenyl)ethynylphenol into 2-phenylbenzofuran at 110° C. with toluene as a solvent, with a yield of 72%. According to the market price of the iridium catalyst, the cost of ...

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