A kind of method and application thereof for preparing 2-aryl malonamide

Abstract

The invention provides a method for preparing 2-aryl malonamide and application thereof. According to the method, 2-(cyclohexadienylidene)malononitrile is used as a raw material and undergoes an aromatization-hydrolysis reaction under the action of an oxidizing agent and water so as to obtain 2-arylmalonamide in one step. Compared with the prior art, the method for preparing 2-arylmalonamide provided by the invention has the following remarkable features and advantages: (1) completely different synthesis strategies are adopted; (2) the raw material is simple and easily available; and (3) yieldis high, the use of expensive metal catalysts is avoided, cost is low, and the method is suitable for industrial production.

Description

technical field

[0001] The invention belongs to the field of organic synthesis, and in particular relates to a preparation method and application of 2-aryl malonamide. Background technique

[0002] 2-Arylmalonamide compounds are an important class of intermediates in organic synthesis. For example, 2-(2,6-diethyl-4-methylphenyl)malonamide is an important intermediate for the preparation of the highly effective herbicide pinoxaden (WO000 / 78881, WO 00 / 78712).

[0003] The current method for synthesizing 2-aryl malonamide compounds is mainly to prepare by hydrolysis of 2-aryl malononitrile compounds (WO 00 / 78712). This method has the problem that the raw material 2-aryl malononitrile compound is difficult to prepare, especially the preparation of the 2-(2,6-disubstituted aryl) malononitrile raw material with large steric hindrance. The best way to synthesize 2-(2,6-disubstituted aryl) malononitriles is to use the corresponding aromatic amine compounds as raw materials, follow...

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