Synthesis method of ethyl 4-cyano-3-hydroxybutyrate

Abstract

The invention provides a synthesis method of ethyl 4-cyano-3-hydroxybutyrate, and relates to the technical field of ethyl butyrate synthesis. The synthesis method comprises the following steps: performing reaction synthesis: adding deionized water into a reaction flask, adding ethyl 4-chloro-3-hydroxybutyrate, adding a buffer agent to regulate the pH value to 6.9-7.1, adding dehalogenase, introducing hydrocyanic acid, adding the buffer agent again to regulate the pH value to 6.9-7.1, wherein the reaction temperature is 40-55 DEG C, performing reacting until the content of ethyl 4-chloro-3-hydroxybutyrate is analyzed to be less than or equal to 1%, then carrying out plate dotting again to confirm that the reaction is complete, and confirming a reaction end point to obtain a reaction solution; and then carrying out steps of desolvation and water removal, filtration and desalting, extraction and washing, and desolvation and rectification subsequentially. Compared with the prior art, the synthesis method has the advantages that the cost of links such as three-waste treatment, equipment investment and manual investment is reduced, and the technical advancement of the product is improved.

Description

technical field [0001] The invention relates to the technical field of ethyl butyrate synthesis, in particular to a synthesis method of ethyl 4-cyano-3-hydroxybutyrate. Background technique [0002] Ethyl 4-cyano-3-hydroxybutyrate is the key intermediate of atorvastatin. Atorvastatin is a selective inhibitor of HMG-CoA reductase, mainly used to reduce plasma cholesterol and lipoprotein levels, and can pass Increasing the level of low-density lipoprotein (LDL) on the surface of liver cells is a commonly used cardiovascular drug for regulating blood lipids. [0003] The synthetic technique of ethyl cyano-3-hydroxybutyrate is as follows at present: [0004] [0005] The disadvantages of the existing synthetic process route are as follows: [0006] (1) This synthetic route sodium cyanide consumption is big, and utilization rate is low, and molar proportion is 1.6-1.8 times of 4--chloro-3-hydroxybutyrate ethyl ester, produces a large amount of cyanide-containing waste water,...

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Problems solved by technology

[0006] (1) This synthetic route sodium cyanide consumption is big, and utilization rate is low, and molar ratio is 1.6-1.8 times of 4--chloro-3-hydroxybutyrate ethyl ester, produces a large amount of cyanide-containing waste water, and treatment cost is high;

[0007] (2) The synthetic route extractant uses a large amount, the number of extractions is many, and the operating cost is high;

[0008] (3) The reaction control of this synthetic route requires a pH value of 6.9±0.1, which requires high reaction control and high operating costs;

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