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Buflomedil production method

A technology of buflomedil and pyrrolidine, which is applied in the field of preparation of buflomedil, can solve problems such as high toxicity, and achieve the effects of short reaction time, high reaction yield and good product quality

Inactive Publication Date: 2008-07-16
QILU TIANHE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This route is very toxic because of the use of the organic solvent benzene

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0028] Put 50g of 4-chloro-1-(2,4,6-trimethoxyphenyl)butanone, 27g of pyrrolidine, 150g of cyclohexane, and 0.85g of sodium iodide into a 1000ml reaction flask successively, heat to reflux, and keep the temperature for reaction. After 5 hours, the temperature was lowered to 35°C, and the organic layer was washed three times with 150 ml of 20% sodium chloride solution, and then the organic layer was depressurized and concentrated to obtain 50.7 g of buflomedil with a content of 99.0% (HPLC). The yield was 90.24%.

Embodiment 2

[0030] Put 50g of 4-chloro-1-(2,4,6-trimethoxyphenyl)butanone, 30g of pyrrolidine, 250g of cyclohexane, and 0.85g of sodium iodide into a 1000ml reaction flask in sequence, heat to reflux, and keep the temperature for reaction. After 9 hours, the temperature was lowered to below 35°C, and the organic layer was washed three times with 150ml of 20% sodium chloride solution, and then the organic layer was depressurized and concentrated to obtain 52.52g of buflomedil with a content of 98.5% (HPLC). The yield was 93.5%.

Embodiment 3

[0032] Put 50g of 4-chloro-1-(2,4,6-trimethoxyphenyl)butanone, 18g of pyrrolidine, 300g of cyclohexane, and 0.85g of sodium iodide into a 1000ml reaction flask in sequence, heat to reflux, and keep the reaction temperature warm. After 12 hours, the temperature was lowered to below 35°C, and the organic layer was washed three times with 150 ml of 20% sodium chloride solution, and then the organic layer was depressurized and concentrated to obtain 50.7 g of buflomedil with a content of 98.5% (HPLC). The yield was 90%.

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Abstract

The invention discloses a preparation method for buflomedil, which adopts a 4-fluoro-1-(2, 4, 6-trimethoxybenzene) butanone and a pentazane as raw materials. In an organic solvent cyclohexane, a sodium iodide is adopted as a catalyst to derive a buflomedil with a reaction temperature from 20 DEG C to a boiling point of a solvent system. The preparation method for buflomedil of the invention has the advantages of safety, reliability, shorter reaction time, ideal yield and product purity.

Description

Technical field [0001] The invention relates to a method for synthesizing a compound, in particular to a method for preparing buflomedil. Background technique [0002] The structural formula of buflomedil hydrochloride is as follows: [0003] [0004] It is a vasodilator developed by Lafon in France to treat encephalopathy and peripheral vascular disorders. Buflomedil hydrochloride is a vasoactive compound with multiple pharmacological effects: blocking α-adrenergic receptors, relaxing vascular smooth muscle, inhibiting platelet aggregation, improving microcirculation, increasing and improving red blood cell deformability and filtration, and reducing Blood viscosity and so on. At present, it is widely used clinically to treat ischemic cerebrovascular disease, vascular dementia and peripheral vascular disease. [0005] According to literature reports, the synthetic routes of buflomedil are mainly summarized into three: [0006] 1. U.S. Patent (US3895030) reports: Taking 4-chloro...

Claims

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Application Information

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IPC IPC(8): C07D295/104A61K31/4015A61P9/08A61P9/10
CPCC07D295/108A61P9/08A61P9/10
Inventor 魏蒲仁陈中南杜召新
Owner QILU TIANHE PHARMA
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