Technology for industrialized production of hydrochloric acid multi-donepezil

A technology of donepezil hydrochloride and a process method, which is applied in the process field of industrialized production of donepezil hydrochloride, can solve the problems of high product impurities, low product yield, and high raw material cost, and achieve the effects of simplified operation procedures, reasonable process design, and improved product purity

Inactive Publication Date: 2004-09-01
TIANJIN LISHENG PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is found through experiments that the reproducibility of the final reduction step of its process is very poor, and there are mainly the following problems: (1) the product has many impurities (crude product contains 5%), and it is separated and purified by column chromatography, which is not suitable for industrialized production; (2) the product is collected. The rate is low and unstable, and the cost of raw materials is high; (3) using platinum dioxide catalyst, it is troublesome to recycle
Therefore, it brings great difficulties to the industrialized production of products

Method used

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  • Technology for industrialized production of hydrochloric acid multi-donepezil
  • Technology for industrialized production of hydrochloric acid multi-donepezil
  • Technology for industrialized production of hydrochloric acid multi-donepezil

Examples

Experimental program
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Embodiment

[0025] 1. Preparation of 5,6-dimethoxy-2-(4-piperidinylmethyl)-indan-1-one acetate

[0026] (1) Reaction formula:

[0027]

[0028] (2) Feeding amount and mole number:

[0029] (I) 3.0g (0.011Mol)

[0030] Palladium / carbon 0.3g(W / W10%)

[0031] Absolute ethanol 60ml (V / W 20 times)

[0032] Acetic acid 0.7ml (0.012Mol)

[0033] (3) Operation:

[0034] Use a 100 ml autoclave, put in the above raw materials, ventilate three times, 80-100 ° C, 2.0 MPa pressure, stir the reaction, hydrogen absorption reaches the theoretical amount, filter out palladium / carbon, and the HPLC content is ≥ 97%.

[0035] (4) Recovery of solvents and treatment of three wastes:

[0036] Palladium / carbon continues to be used and can be applied several times.

[0037] The ethanol reaction solution was directly used in the next reaction.

[0038] The preparation method of raw material (I) refers to J.Heter.Chem.2(4)366,1965.

[0039] 2. Preparation of (±) 2,3 dihydro-5,6-dimethoxy-2-{[(1-benzyl)-...

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PUM

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Abstract

The invention relates to the industrial production method of donepezil HCL, wherein 5,6-dimethoxyl-2-(4-piperidine methyl)- dihydroindene-1-ketone acetate is first prepared through a reduction reaction with the reaction condition being, pressure: 0.5-5.0 MPa, temperature: 25-150 deg. C, time: 2-5 hours, reducing agent: palladium-carbon, raw material: palladium-carbon : solvent W:W:V = 1:0.1:20, then (+-)2,3 dihydro-5,6-dimethoxy-2-{[(1- benzyl)-4- piperidino] methyl}-1H- indene- ketone hydrochlorate is prepared through a substitution reaction with the reaction condition being, the mol ratio of raw material : benzyl chloride : deoxidizing agent = 1:1.1:2.2, temperature: 40-100 deg. C, solvent: methanol, ethanol or isopropanol.

Description

Technical field [0001] The invention relates to a production process of donepezil hydrochloride, in particular to a process for industrialized production of donepezil hydrochloride. Background technique [0002] Donepezil hydrochloride is an acetylcholinesterase inhibitor developed by Japan's Eisai Company for the treatment of Alzheimer's dementia (AD). It has been reported in the literature that there are several synthesis methods, but due to harsh reaction conditions, special reagents and intellectual property rights are required. , not suitable for localization. [0003] Germany Bayer applied for European patent (EP0711756A1) in 1996, and disclosed the reaction formula as: [0004] [0005] (Donepezil Hydrochloride) [0006] Compared with the previous methods, the above-mentioned process method uses raw materials and reaction conditions that are more suitable for my country's national conditions, and there is no problem of intellectual property rights. However, it i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/22
Inventor 瞿虹田青松张殿镇刘文华李天昌崔丽霞陶孝铮刘遵利贺春蕊
Owner TIANJIN LISHENG PHARM CO LTD
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