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Preparing method for entacapone A-type crystals

A technology of entacapone and alkanol, which is applied in the field of preparation technology of entacapone A-type crystal, can solve the problems of long crystallization time, high production cost, strong irritation, etc., and can improve yield and reduce production. Comprehensive cost and effect of simplifying post-processing procedures

Inactive Publication Date: 2015-11-18
ZEIN BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The solvent used in this method is highly irritating to the human body, has high toxicity, and takes a long time for crystallization, resulting in high production costs and other shortcomings.

Method used

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  • Preparing method for entacapone A-type crystals
  • Preparing method for entacapone A-type crystals
  • Preparing method for entacapone A-type crystals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 Preparation of Entacapone Type A Crystal

[0032] Take 100.0g of entacapone crude product, put 1000ml of absolute ethanol into a three-necked bottle, heat to reflux and dissolve under stirring, cool down to 20~40°C in 30~40min, cool down to 0~10°C in 20~35min, and filter with suction. The filter cake was dried under reduced pressure at 40°C to obtain 93.9 g of yellow powder, with a yield of 93.9%.

Embodiment 2

[0033] Embodiment 2 Preparation of Entacapone Type A Crystal

[0034] Take 100.0g of entacapone crude product, put 1000ml of 95% ethanol into a three-necked flask, heat to reflux and dissolve under stirring, cool down to 20~40°C in 30~40min, cool down to 0~10°C in 20~35min, filter with suction, filter The cake was dried under reduced pressure at 40°C to obtain 95.0 g of yellow powder with a yield of 95.0%.

Embodiment 3

[0035] Embodiment 3 Preparation of Entacapone Type A Crystal

[0036] Take 100.0g of entacapone crude product, put 1200ml of isopropanol into a three-necked flask, heat it to reflux and dissolve it under stirring, cool down to 20~40°C in 30~40min, cool down to 0~10°C in 20~35min, and filter with suction. The filter cake was dried under reduced pressure at 55°C to obtain 92.0 g of yellow powder with a yield of 92.0%.

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Abstract

The invention discloses a preparing method for entacapone A-type crystals. The preparing method includes the step that entacapone is recrystallized with C1-C4 alkanol or water-containing C1-C4 alkanol as solvents. The preparing method has the advantages that the solvents are low in toxicity, operation is easy, the operation time is short, cost is low, and products are high in yield and good in quality; the preparing method is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and relates to a preparation process of entacapone type A crystal, which is a medicinal crystal form of entacapone. Background technique [0002] Entacapone belongs to catechol-O-methyltransferase (COMT) inhibitors, it is a reversible, specific COMT inhibitor that mainly acts on the periphery, and it is used simultaneously with levodopa preparations. This product reduces the metabolism of levodopa to 3-oxo-methyldopa (3-OMD) by inhibiting the COMT enzyme, which increases the bioavailability of levodopa and increases the total amount of levodopa available in the brain. This effect has been confirmed in clinical trials. Clinical trials have shown that the addition of levodopa to this product can prolong the "on" time by 16%, and shorten the "off" time by 24%. This product mainly inhibits COMT in surrounding tissues. The COMT inhibitory effect in red blood cells is closely related t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C255/41C07C253/34
Inventor 王飞邓祥林罗礼平代毅谢侨余佳黄燕梅刘小伟
Owner ZEIN BIOTECHNOLOGY CO LTD
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