Method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions

Abstract

The invention discloses a method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions. According to the method, glacial aceticacid is taken as a catalyst; at solvent-free room temperature conditions, physical grinding is adopted, reaction of 2-substituted arylamines (2-mercapto arylamine, 2-aminophenol, and o-phenylenediamine) and aromatic aldehydes is carried out using physical grinding. The method is friendly to the environment, is simple in operation, is safe, is low in cost, and is high in efficiency. Compared withthe prior art, the advantages are that: the method is suitable for a large amount of functional groups, yield is high, less by-product is generated, operation is simple, the method is safe, cost is low, and the method is friendly to the environment.

Description

technical field [0001] The invention discloses a method for rapidly preparing benzoheterocyclic compounds by using a physical grinding method under the condition of room temperature without solvent. Background technique [0002] Benzoheterocyclic compounds have unique physiological and biological activities in medicine, have excellent antimicrobial activity, have good vasopressin antagonistic activity and can be used as vasodilators, hypotensive drugs, water diuretics, platelet aggregation Inhibitors etc. The modification of benzoheterocyclic compounds is mainly to introduce different substituents on the benzene ring or introduce different active groups on the 2-position, so the synthesis of multi-substituted benzoheterocyclic derivatives is the most popular research in the synthesis of such compounds. part of attention. (1) At present, benzothiazole and its derivatives are synthesized industrially: a. The arylamine is treated with cyanogen sulfide to undergo electrophilic...

AI Technical Summary

Problems solved by technology

The synthesis reactions of the above heterocyclic compounds all use solvents to varying degrees, the reaction time is long, the preparation process is cumbersome, the cost is relatively high, and the reaction yield is often reduced due to the occurrence of side reactions.

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