A kind of method for the synthesis of benzimidazole derivatives catalyzed by N,N-dimethylaminothioformyl chloride derivatives under microwave radiation

Abstract

The invention discloses a method for catalytic synthesis of benzimidazole derivative under microwave radiation. The method comprises steps as follows: the catalytic quantities of a catalyst cuprous iodide, an aided catalyst sodium hydroxide, o-phenylenediamine, a derivative of o-phenylenediamine and an N,N-dimethylthiocarbamoyl chloride derivative are added to a reaction vessel and taken as raw materials, a pyridine solvent is added, all materials are placed in a microwave reaction instrument and subjected to a reaction at certain temperature and power, after a period of time, reduced-pressureconcentration is performed, and a product is subjected to column chromatography purification. The efficient method which adopts the novel raw materials and is simple and convenient to operate and used for preparing the benzimidazole derivative is provided. Compared with the prior art, the method has the advantages of being simple to operate, high in yield, safe, low in cost and environmentally friendly, reaction speed is obviously higher than that of conventional heating, and reaction conditions are mild.

Description

technical field [0001] The invention relates to a method for preparing benzimidazole derivatives. That is, using substituted o-phenylenediamine and N,N-dimethylaminothioformyl chloride derivatives as raw materials, introducing microwave as an auxiliary synthesis method, and efficiently catalyzing and rapidly preparing benzimidazole derivatives. Background technique [0002] Benzimidazole and its derivatives, as a class of nitrogen-containing fused heterocyclic compounds, are fused by aromatic rings and imidazole rings. It has a special status in the field of organic chemistry. It is a class of heterocyclic compounds with potential anticancer and bactericidal biological activities. In medicinal chemistry, benzimidazole has always been an important pharmacophore. Compounds containing benzimidazole structures are widely used in antibacterial, antiulcer, antihypertensive, antiviral, anticancer, antiparasitic and antihistamine, and their synthesis research has far-reaching signi...

AI Technical Summary

Problems solved by technology

The currently reported synthesis methods of benzimidazole compounds have their own advantages and disadvantages, and their use is more or less limited due to the difficulty in obtaining raw materials, the high toxicity of some reagents, the severe reaction conditions and serious environmental pollution.

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