Preparation method of gemfibrozil

A preparation step, sodium ethoxide technology, applied in the preparation of organic compounds, carboxylate preparation, chemical instruments and methods, etc., can solve the problems of high price, increased production cost, unsuitable raw materials, etc., and achieves easy purchase and cost saving. , the effect of saving workload

Active Publication Date: 2016-06-22
KAMP PHARMA
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  • Claims
  • Application Information

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Problems solved by technology

[0003] Explanation of the closest scheme: Condensation reaction of 2,5-xylenol (1) with 5-halo-2,2-dimethylvalerate in the presence of a base under the action of a phase transfer catalyst, followed by addition of base Carry out the hydrolys

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  • Preparation method of gemfibrozil
  • Preparation method of gemfibrozil
  • Preparation method of gemfibrozil

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[0040] The following examples are only to further illustrate the present invention, and do not limit the present invention in any form.

[0041] (1) Preparation of (IV):

[0042] Add the reactant (I) (122g, 1mol), (III) (160g, 1mol), methanol (500mL) into the reaction flask, lower the temperature to about 0°C, and add sodium methoxide (113g, 2.1mol) Add to the above reaction flask in batches, after the addition, stir and react at 0°C for 1h, then add (II) (200g, 1mol) and heat up to reflux temperature, react for 24h, monitor by TLC, after the reaction is complete, set the temperature Reduce to room temperature, add KOH (67.0g, 1.2mol) aqueous solution, stir for 4 hours, then cool to 0°C in an ice bath, add 2mol / L hydrochloric acid to adjust the pH to about 1, heat up to 90°C, and stir for reaction After 2.5 hours, the temperature was lowered to 0°C to precipitate a large amount of white solid powder, which was filtered, washed with water, and the filter cake was dried under r...

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Abstract

The invention provides a preparation method of gemfibrozil. The preparation method is characterized by comprising the following steps: carrying out a salt-forming reaction between starting materials, namely 2,5-dimethylphenol and diethyl malonate, under the action of alkali; carrying out a nucleophilic substitution between the reaction product and 1,3-dibromopropane; hydrolyzing in an aqueous solution of alkali and carrying out a decarboxylation reaction to generate 5-(2,5-dimethylphenoxyl)pentanoic acid; and carrying out a methylation reaction between the reaction product and dimethyl sulphate (V) under the action of alkali so as to generate gemfibrozil. The preparation method has simple processing steps, reaction conditions are not harsh, synthesis route has no special requirements on equipment, investment cost of production equipment is greatly reduced, and it is easy to realize industrial production. The raw materials are easily available in the market, and cost is relatively low. Thus, industrial cost reduction is realized.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, and in particular relates to a preparation method of gemfibrozil. Background technique [0002] Gemfibrozil (Gemfibrozil) chemical name is 2,2-dimethyl-5-(2,5-dimethylphenoxy) valeric acid, which belongs to clofibrate derivatives blood lipid regulating drugs, and was introduced by the United States in 1982 Years of development and listing. It is suitable for patients with severe type Ⅳ or Ⅴ hyperlipoproteinemia, high risk of coronary heart disease, but diet control, weight loss and other treatments are ineffective. The drug can be used to prevent arteriosclerosis, and help reduce the incidence of myocardial infarction, with less toxic side effects. [0003] Description of the closest scheme: Condensation reaction of 2,5-xylenol (1) with 5-halo-2,2-dimethylpentanoate in the presence of a base under the action of a phase transfer catalyst, followed by addition of a base Carry out the hydrolysis...

Claims

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Application Information

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IPC IPC(8): C07C59/68C07C51/353
Inventor 曾培安刘达吴健民周江
Owner KAMP PHARMA
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