Method for synthesizing benzoxazole through microwave radiation of benzamide compound in water phase

A technology for benzamide and benzoxazole, which is applied in the field of synthesizing benzoxazole from benzamide compounds, can solve the problems of energy and environmental burden, poor biodegradability, long reaction time and the like, and achieves environmental friendliness and easy operation. , the effect of simple operation

Inactive Publication Date: 2019-02-22
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In traditional organic synthesis, it is usually necessary to maintain a high temperature, a long reaction time, and use toxic and poorly biodegradable organic reagents as solvents. This process will undoubtedly impose a huge burden on energy and the environment.

Method used

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  • Method for synthesizing benzoxazole through microwave radiation of benzamide compound in water phase
  • Method for synthesizing benzoxazole through microwave radiation of benzamide compound in water phase
  • Method for synthesizing benzoxazole through microwave radiation of benzamide compound in water phase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Benzoxazole: add 2 ml of water, 1 mmol of benzamide and 0.2 mmol of cesium carbonate in a microwave reactor, react for 10 min in a microwave power of 120 W, extract with ethyl acetate, concentrate under reduced pressure, and the product Silica gel column separation gave a white solid in 99% yield.

Embodiment 2

[0020] Embodiment 2: 2-methylbenzoxazole: the preparation method is the same as that of embodiment 1, and what is added is N - methylbenzamide as a white solid in 93% yield.

Embodiment 3

[0021] Embodiment 3: 2-ethyl benzoxazole: preparation method is the same as embodiment 1, what is added is N - Ethylbenzamide as a white solid in 92% yield.

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Abstract

The invention discloses a method for synthesizing benzoxazole through microwave radiation of a benzamide compound in a water phase. The benzamide compound is added into the water phase under the microwave condition to be subjected to a cyclization reaction for generating the benzoxazole under the alkali condition, and the method for preparing the benzoxazole is environmentally friendly, easy and convenient to operate, safe, low in cost and efficient. Compared with the prior art, the method can be applied to a large number of functional groups, the yield is high, the number of by-products is small, and the method is easy to operate, safe, low in cost and environmentally friendly. (Please see the specifications for the formula).

Description

technical field [0001] The invention belongs to a method for synthesizing benzoxazole by using a benzamide compound under microwave conditions in an aqueous phase. Background technique [0002] Benzoxazoles are a very important class of nitrogen-containing fused heterocyclic compounds, which are important precursors and precursors for organic synthesis. Important role Currently reported methods for synthesizing benzoxazole compounds are rare. Generally speaking, there are two synthetic methods: one is to use nitrobenzene as an oxidant, and o-aminophenol and benzaldehyde are heated and refluxed. The method has high temperature, low yield and many by-products, which limit its development; the other is that in the presence of a dehydrating agent, o-aminophenol and carboxylic acid are condensed. This method uses a large amount of dehydrating agent, and the post-processing is more troublesome. . [0003] Since the concept of "green chemistry" was put forward in 1991, the greeni...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D263/56C07D263/57C07D263/58C07D413/04C07D417/04
CPCC07D263/56C07D263/57C07D263/58C07D413/04C07D417/04
Inventor 甘陈灵许贻文张鹏邹玉莲王津林媚陈艳周孙英
Owner FUJIAN MEDICAL UNIV
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