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Method for preparing donepezil by virtue of simulated moving bed chromatographic separation

A technology for simulating moving bed and donepezil, which is applied to the field of separation and preparation of donepezil by simulated moving bed chromatography, can solve the problems of ineffective utilization and no technical method for separating donepezil enantiomers, etc., and achieves the effects of stable and reliable product and simple process.

Inactive Publication Date: 2015-04-29
NINGBO UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although chromatography and capillary methods have technical advantages in micro-volume separation and analysis, this preparation method cannot be effectively utilized in practical industrial production
[0006] At present, there is no technical method related to the separation of donepezil enantiomers by simulated moving bed chromatography

Method used

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  • Method for preparing donepezil by virtue of simulated moving bed chromatographic separation
  • Method for preparing donepezil by virtue of simulated moving bed chromatographic separation

Examples

Experimental program
Comparison scheme
Effect test

specific example example 1

[0035] operating conditions

[0036] Mobile phase: absolute ethanol

[0037] Flow rate: 1ml / min

[0038] Injection concentration: Donepezil racemate: 0.2mg / ml

[0039] Injection liquid flow rate: v F =0.1ml / min

[0040] Mobile phase flow rate: v D =1.0ml / min

[0041] Flushing fluid flow rate: v P =2.0ml / min

[0042] F pump pressure: 6.8MPa

[0043] P pump pressure: 7.5MPa

[0044] D pump pressure: 7.1MPa

[0045] Switching time: 450s

[0046] Column temperature: 25°C

[0047] Finished product analysis

[0048] The composition of extract and raffinate was analyzed by chiral column Chiralcel-OJ. The content of L-donepezil or D-donepezil is 100%, 95.5%.

specific Embodiment 2

[0049] operating conditions

[0050] Mobile phase: absolute ethanol

[0051] Flow rate: 1ml / min

[0052] Injection concentration: Donepezil racemate: 0.2mg / ml

[0053] Injection liquid flow rate: v F =0.1ml / min

[0054] Mobile phase flow rate: v D =1.0ml / min

[0055] Flushing fluid flow rate: v P =2.0ml / min

[0056] F pump pressure: 6.2MPa

[0057] P pump pressure: 8.1MPa

[0058] D pump pressure: 6.7MPa

[0059] Switching time: 480s

[0060] Column temperature: 25°C

[0061] Finished product analysis

[0062] The composition of extract and raffinate was analyzed by chiral column Chiralcel-OJ. The content of L-donepezil or D-donepezil is 100%, 84.5%.

specific Embodiment 3

[0063] operating conditions

[0064] Mobile phase: absolute ethanol

[0065] Flow rate: 1ml / min

[0066] Injection concentration: Donepezil racemate: 0.2mg / ml

[0067] Injection liquid flow rate: v F =0.1ml / min

[0068] Mobile phase flow rate: v D =1.0ml / min

[0069] Flushing fluid flow rate: v P =2.0ml / min

[0070] F pump pressure: 6.6MPa

[0071] P pump pressure: 7.5MPa

[0072] D pump pressure: 6.8MPa

[0073] Switching time: 510s

[0074] Column temperature: 25°C

[0075] Finished product analysis

[0076] The composition of extract and raffinate was analyzed by chiral column Chiralcel-OJ. The content of L-donepezil or D-donepezil is 100%, 100%.

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Abstract

The invention discloses a method for preparing donepezil by virtue of simulated moving bed chromatographic separation. A laevo isomer and a dextro isomer are separated out from the donepezil by adopting a chiral column Chiralcel-OJ and taking silica gel coated with cellulose-tri(4-methyl benzoate) as a stationary phase and absolute ethyl alcohol as a moving phase. Due to the continuity of the simulated moving bed chromatographic separation, the production efficiency can be greatly improved and the production cost can be reduced; the whole separation process does not involve with any toxic solvent.

Description

technical field [0001] The invention relates to a chiral drug resolution technology, in particular to a method for preparing donepezil through simulated moving bed chromatographic separation. Background technique [0002] The chemical name of donepezil is (±) 2,3-dihydroxy-5,6-bismethoxy-2-{[1-(phenylmethyl)-4-piperidinyl]methyl}-1H-indene- 1-Keto hydrochloride. Studies have shown that donepezil hydrochloride is a long-acting symptomatic drug for Alzheimer's disease (AD). AD is an acquired mental decline with memory loss as the main manifestation and other cognitive impairments. [0003] Donepezil hydrochloride is a second-generation cholinesterase (ChE) inhibitor. Its therapeutic effect is to inhibit the degradation of acetylcholine by acetylcholinesterase and activate the central choline system, thereby reducing neuronal degeneration caused by impaired cholinergic transmission. Thereby protecting and improving the function of nerve cells related to learning and memory. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/32
CPCC07D211/32
Inventor 刘望才金崇君彭革朱瑞芬罗胜亮赵应松
Owner NINGBO UNIVERSITY OF TECHNOLOGY
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