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Method for preparing donepezil hydrochloride

A technology of donepezil hydrochloride and reaction, applied in the field of preparation of donepezil hydrochloride, can solve the problems of being unsuitable for industrialized production, difficult in industrialized production, and high cost of raw materials, and achieve the effects of reducing equipment investment, shortening reaction time, and improving product purity

Inactive Publication Date: 2011-05-18
TIANJIN BIJIA PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0008] The above-mentioned process mainly has the following problems: (1) the product has many impurities (the crude product contains 5%), and it is separated and purified by column chromatography, which is not suitable for industrial production; (2) the product yield is low and unstable, and the cost of raw materials is high; ( 3) Use platinum dioxide catalyst, recovery trouble
Therefore, it brings great difficulties to the industrialized production of products

Method used

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  • Method for preparing donepezil hydrochloride
  • Method for preparing donepezil hydrochloride
  • Method for preparing donepezil hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0033] 1. Preparation of 5,6-dimethoxy-2-(4-piperidinylmethyl)-indan-1-one acetate

[0034] (1) Reaction formula:

[0035]

[0036] (2) Feeding amount and mole number:

[0037]

[0038] (3) Operation:

[0039] Use a 100ml autoclave, put in the above raw materials, ventilate three times, 80-100°C, 2.0MPa pressure, stir the reaction, hydrogen absorption reaches the theoretical amount, filter out palladium / carbon, and the HPLC content is ≥ 97%.

[0040] (4) Recovery of solvents and treatment of three wastes:

[0041] Continue to use Raney nickel, can be applied several times.

[0042] Preparation of Ni-W-2

[0043] Dissolve 800g of NaOH in 3000ml of water and add to the reaction tank, add 650g of Ni-Al alloy at 10°C, and raise the temperature to room temperature. When the hydrogen gas is generated slowly, reheat, and when the hydrogen gas is violently generated, stop heating, remove the water, add NaOH aqueous solution to stir, stand still, remove the supernatant, wash...

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Abstract

The invention discloses a method for preparing donepezil hydrochloride. The method prepares the donepezil hydrochloride by five steps of reduction reaction for preparing 5,6-dimethoxy-2-(-4-piperidine methyl)-indane-1-ketone acetate, condensation, reduction, substitution and closed ring decarboxylation. The preparation method has the advantages of easily obtained and cheap raw materials, simple synthesis operation, mild reaction conditions, good reaction selectivity and good yield, and is easy to control and suitable for industrialized production.

Description

technical field [0001] The invention relates to a production process of donepezil hydrochloride, in particular to a preparation method of donepezil hydrochloride. Background technique [0002] Donepezil Hydrochloride (Aricept) is a highly selective, long-acting and reversible acetylcholinesterase inhibitor developed by Japan Eisai Co., Ltd. for the treatment of mild to moderate Alzheimer's disease. The drug has the characteristics of good curative effect, high safety, and convenient administration; it mainly increases the concentration of the neurotransmitter acetylcholine by inhibiting the activity of acetylcholinesterase in the brain, thereby improving symptoms such as memory loss and life ability decline in senile dementia patients . Aricept was first approved by the US Food and Drug Administration and the British Medicines Agency in 1996, and is currently listed in more than 40 countries and regions around the world. [0003] Donepezil hydrochloride is a long-acting dr...

Claims

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Application Information

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IPC IPC(8): C07D211/32
Inventor 范培柱
Owner TIANJIN BIJIA PHARMA CO LTD
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