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

A technology of grinding method and conditions, applied in the direction of organic chemistry, etc., can solve the problems of complicated preparation process, reduced reaction yield, long reaction time, etc., and achieves the effects of simple operation, low cost and easy operation.

Inactive Publication Date: 2019-01-11
FUJIAN MEDICAL UNIV
View PDF1 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions
  • Method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions
  • Method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: 2-phenylbenzimidazole: Add catalytic amount of 1 ml of glacial acetic acid, 1 mmol of o-phenylenediamine, and 1.2 mmol of benzaldehyde in a mortar and grind it rapidly for 10 minutes at room temperature, then use ethyl acetate and water The product was extracted and concentrated under reduced pressure. The product was purified by column chromatography to obtain a white solid with a yield of 93%.

Embodiment 2

[0028] Example 2: 2-(4-methylphenyl)benzimidazole: the preparation method is the same as in Example 1, adding 4-methylbenzaldehyde instead of benzaldehyde (the same as in Example 3-29) to obtain a white solid with a yield of 91%.

Embodiment 3

[0029] Example 3: 2-(4-ethylphenyl)benzimidazole: the preparation method is the same as in Example 1, adding 4-ethylbenzaldehyde to obtain a light yellow solid with a yield of 92%.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/18C07D263/57C07D277/66
CPCC07D235/18C07D263/57C07D277/66
Inventor 柯方许贻文张鹏林媚陈艳周孙英
Owner FUJIAN MEDICAL UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap