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Production method of cilostazol

A production method and a technology for cilostazol, which are applied in the field of drug preparation, can solve the problems of high production cost and complicated production process, and achieve the effects of low production cost and convenient and simple production.

Inactive Publication Date: 2015-07-01
张云
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the current production of cilostazol, the manufacturing process is complicated and the production cost is high

Method used

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Embodiment Construction

[0006] Now in conjunction with the present invention for further detailed description.

[0007] A kind of production method of cilostazol of the present invention, concrete steps are as follows: take 5-chloro-N-cyclohexylpentanamide as raw material, under ice bath cooling, add 1.75g5-chloro-N-cyclohexylpentanamide to Add 1.9 g of phosphorus pentachloride slowly to a solution of 15 ml of benzene, then stir at room temperature for 1 h, then add a solution of 1.4 mol / L H3N in 1 ml of benzene with stirring at room temperature, stir overnight, then reflux for 2 h, evaporate under reduced pressure Remove the solvent, pour the residue into ice water, extract with chloroform, wash the extract with water, dilute sodium bicarbonate solution and water successively, dry over anhydrous sodium sulfate, evaporate the chloroform, and recrystallize the residue with isopropanol-water to obtain 1.7g of 5-(4-chlorobutyl)-1-cyclohexyltetrazole, 3.2g of 6-hydroxy-3,4-dihydro-2(1H)-quinolinone and 1...

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PUM

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Abstract

The invention relates to a production method of cilostazol. The method comprises the specific steps of: slowly adding 1.9g of phosphorus pentachloride into 1.75g of a raw material 5-chloro-N-cyclohexyl valeramide in 15ml of benzene solution, adding 1.4 mol / L H3N in 11 ml of benzene solution to obtain 1.7g of 5-(4-chlorobutyl)-1-cyclohexyl tetrazolium, dissolving 3.2g of 6-hydroxy-3,4-two-dihydro-2(1H)-quinolinone and 1.4g of potassium hydroxide in 20ml of isopropanol, extracting with, followed by 1 mol / L sodium hydroxide solution, dilute hydrochloric acid and water washing, conducting silica gel chromatography on residual liquid, eluting with chloroform methanol (30:1), recrystallizing with methanol-water to obtain 6.0g of colorless acicular crystal cilostazol. The production method of cilostazol has low manufacture cost and convenient production, and can realize batch production.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a production method of cilostazol. Background technique [0002] Cilostazol has vasodilator effect and anti-platelet function, and is used for the treatment of chronic arterial occlusion caused by atherosclerosis, Takayasu arteritis, obliterative thromboangiitis (thromboangiitis obliterans), and diabetes disease. This drug can improve chronic ulcers, pain, cold sensation and intermittent claudication caused by limb ischemia, and can be used as a supplementary treatment after angioplasty, vascular grafting and sympathectomy to help relieve symptoms, improve circulation and inhibit Thrombosis in graft vessels. Due to the current production of cilostazol, the manufacturing process is complicated and the production cost is high. Contents of the invention [0003] The technical problem to be solved by the present invention is: in order to overcome the above-mentioned problems,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 张云
Owner 张云
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