Green preparation method of aryl [alpha]-keto ester compound

Abstract

The invention discloses a green preparation method of an aryl [alpha]-keto ester compound. The method comprises the specific steps that an [alpha]-diazo compound serves as a reaction raw material, copper sulfate serves as a catalyst, water serves as a solvent, a target product aryl [alpha]-keto ester compound is prepared through a reaction at the temperature of 60 DEG C, the structural general formula of the [alpha]-diazo compound is shown in the specification, and the structural general formula of the correspondingly prepared target product aryl [alpha]-keto ester compound is shown in the specification. The method for synthesizing the target product aryl [alpha]-keto ester compound by catalyzing the [alpha]-diazo compound derivative with copper sulfate has the advantages that the reactioncondition is green and mild, the catalyst is cheap and easy to obtain, the operation is simple and convenient, the yield is relatively high, the universality of a reaction substrate is wide, and thelike.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a green preparation method of aryl α-keto ester compounds. Background technique [0002] Aryl α-ketoesters are a class of dicarbonyl compounds, which are often used as active intermediates in pesticide research, drug development and organic synthesis, and have a wide range of applications. α-ketoesters and their derivatives have an irreplaceable position in the field of medicine. Under certain conditions, α-ketoesters can be reduced to α-hydroxyl esters, which are amino alcohol ester M receptor antagonists (such as : the basic structure of the drug effect of orphenidium bromide). Whether the carbonyl carbon in α-ketoesters is a potential chiral carbon atom has always been a hot topic in the field of chiral compound research. In addition, α-ketoester is also a synthetic intermediate of many enzyme inhibitors, such as renin inhibitors, cysteine ​​protease in...

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Problems solved by technology

[0003] So far, scientific researchers have discovered many synthetic methods of aryl α-keto esters, but most of the synthetic methods have cumbersome steps, complicated reaction conditions, low yield or use organic toxic solvents or rhodium salts as Catalyst, such as using rhodium catalyst, rhodium is a kind of noble metal, which greatly increases the reaction cost and what the reaction uses is an organic solvent, and a higher yield can be obtained only under reflux state, and this harsh reaction condition limits this synthesis Further application of the method

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