Preparation method of high-purity and low-chroma gemfibrozil

A technology of gemfibrozil and gemfibrozil isobutyl ester, applied in the field of medicinal chemistry, can solve the problems of gemfibrozil unqualified, easy to deteriorate and easy to change color after long-term storage, and achieve pure white color and high quality Requirements, the effect of low chroma
CN105669368BActive Publication Date: 2018-02-06浙江精进药业有限公司

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
浙江精进药业有限公司
Publication Date
2018-02-06

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Abstract

The invention discloses a high-purity low-chroma gemfibrozil preparation method. The method comprises 1, preparing a gemfibrozil isobutyl ester crude product and can also comprises 2, adding an alkali liquor II in the gemfibrozil isobutyl ester crude product until the system pH is in a range of 10.0-12 and carrying out reduced pressure rectification to obtain gemfibrozil isobutyl ester, 3, carrying out reflux alkaline hydrolysis on the gemfibrozil isobutyl ester and carrying out acid adjustment to obtain a gemfibrozil crude product, and 4, refining the gemfibrozil crude product through adding an alcohol-water solution into the gemfibrozil crude product, carrying out heating reflux, carrying out heat preservation for 0.5-1h, carrying out cooling to a temperature of 0-5 DEG C, carrying out thermal insulation stirring for 1.5-2.5h, carrying out filtration to obtain filter cake and drying the filter cake to obtain high-purity low-chroma gemfibrozil.
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Description

technical field

[0001] The invention relates to a preparation method of gemfibrozil with high purity and chromaticity, which belongs to the technical field of medicinal chemistry, and specifically relates to a gemfibrozil with a pure white color, a liquid-phase normalized content of more than 99.9%, and a chromaticity of less than 3.0. The preparation method of gemfibrozil, so that gemfibrozil will not turn red and change color when stored for a long time. Background technique

[0002] Gemfibrozil, the chemical name is 2,2-dimethyl-5-(2,5-dimethylphenyloxy)-pentanoic acid, the English name is 5-(2,5-dimethylphenoxy)-2 ,2-dimethylpentanoic acid, the structural formula is as follows:

[0003]

[0004] Gemfibrozil is a clofibrate blood lipid regulating drug, used for hyperlipidemia, stable drug effect, low adverse reaction rate, high safety, can be taken for a long time, and can prevent arteriosclerosis and help reduce myocardial infarction morbidity. It was launched in t...

Claims

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