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Preparation method of donepezil hydrochloride for treating Alzheimer's disease

A technology for donepezil hydrochloride and Alzheimer's disease, which is applied in the field of preparation of donepezil hydrochloride and can solve problems such as complicated operation methods and the like

Inactive Publication Date: 2017-09-01
芜湖耄智生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] For the above-mentioned prior art, the purpose of the present invention is to overcome the synthesis of donepezil hydrochloride in the prior art with indanone as the main raw material for synthesis. Bring the problem of certain inconvenience to the user, thereby provide a kind of raw material that is easy to get, reaction is simple, the preparation method of donepezil hydrochloride of safe operation

Method used

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  • Preparation method of donepezil hydrochloride for treating Alzheimer's disease
  • Preparation method of donepezil hydrochloride for treating Alzheimer's disease
  • Preparation method of donepezil hydrochloride for treating Alzheimer's disease

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preparation example Construction

[0016] The present invention provides a preparation method of donepezil hydrochloride for the treatment of Alzheimer's disease, wherein the preparation method comprises:

[0017] 1) Mixing 3,4-dimethoxybenzaldehyde and diethyl malonate to prepare a mixture M1 containing a compound represented by formula (I);

[0018] 2) The mixture M1 prepared in step 1) is reacted under ice bath conditions in the presence of sodium borohydride to obtain a mixture M2 containing the compound represented by formula (II);

[0019] 3) Add 4-chloromethylpyridine to the mixture M2 prepared in step 2) to prepare a mixture M3 containing the compound represented by formula (III);

[0020] 4) The mixture M3 prepared in step 3) is subjected to a ring closure reaction to obtain a mixture M4 containing a compound represented by formula (IV);

[0021] 5) Add p-toluenesulfonic acid and hydrochloric acid to the mixture M4 prepared in step 4) to prepare donepezil hydrochloride.

[0022]

[0023] In the present invention,...

Embodiment 1

[0037] 1) Mixing 0.1 mol of 3,4-dimethoxybenzaldehyde, 0.08 mol of diethyl malonate and 10 mL of ethanol, and then reacting for 6 hours at a temperature of 120° C. to prepare a mixture containing formula (I ) The mixture of compounds shown in M1;

[0038] 2) Add 10 mL of ethanol to the mixture M1 prepared in step 1) in the presence of 0.12 mol of sodium borohydride, and react under ice bath conditions to obtain a mixture M2 containing the compound represented by formula (II);

[0039] 3) Add 0.11 mol of 4-chloromethylpyridine and 10 mL of ethanol to the mixture M2 prepared in step 2) to prepare a mixture M3 containing the compound represented by formula (III);

[0040] 4) Under the condition of pH 9, 0.1 mol of polyphosphoric acid was added to the mixture M3 prepared in step 3), and the mixture was reacted at a temperature of 70° C. for 1 hour to prepare a mixture containing as shown in formula (IV) The mixture of the compounds shown M4;

[0041] 5) Add 0.11 mol of p-toluenesulfonic ...

Embodiment 2

[0043] 1) Mix 0.1 mol of 3,4-dimethoxybenzaldehyde, 0.15 mol of diethyl malonate and 10 mL of ethanol, and place the mixture at a temperature of 160° C. for reaction for 12 hours to prepare a mixture containing formula (I ) The mixture of compounds shown in M1;

[0044] 2) Add 10 mL of ethanol to the mixture M1 prepared in step 1) in the presence of 0.16 mol of sodium borohydride, and react under ice bath conditions to obtain a mixture M2 containing the compound represented by formula (II);

[0045] 3) Add 0.15 mol of 4-chloromethylpyridine and 10 mL of ethanol to the mixture M2 prepared in step 2) to prepare a mixture M3 containing the compound represented by formula (III);

[0046] 4) Under the condition of pH 11, 0.12 mol of polyphosphoric acid was added to the mixture M3 prepared in step 3), and the mixture was reacted at a temperature of 100° C. for 2 hours to prepare the mixture as shown in formula (IV) The mixture of the compounds shown M4;

[0047] 5) Add 0.15 mol of p-toluen...

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Abstract

The invention discloses a preparation method of donepezil hydrochloride for treating the Alzheimer's disease. The preparation method comprises the following steps: (1) mixing 3,4-dimethoxy benzaldehyde with diethyl malonate, thus preparing a mixture M1 containing a compound which is as shown in a formula (I); (2) enabling the mixture M1 to react under the presence of sodium borohydride and under an ice-bath condition, thus preparing a mixture M2 containing a compound which is as shown in a formula (II); (3) adding 4-chlorometyhyl pyridine in the mixture M2, thus preparing a mixture M3 containing a compound which is as shown in a formula (III); (4) carrying out ring-closing reaction on the mixture M3, thus preparing a mixture M4 containing a compound which is as shown in a formula (IV); (5) adding para-toluenesulfonic acid and hydrochloric acid in the mixture M4, thus preparing the donepezil hydrochloride. According to the preparation method disclosed by the invention, the effect of preparing the donepezil hydrochloride under the conditions that raw materials are easy to obtain, the reaction is simple and the operation is safe is realized.

Description

Technical field [0001] The invention relates to the preparation field of medicines for treating Alzheimer's disease, and in particular to a preparation method of donepezil hydrochloride. Background technique [0002] Donepezil hydrochloride, as an important drug for the treatment of Alzheimer's disease, has extremely high market value. In the prior art, indenone is often used as the main raw material for synthesis, and the operation method is relatively complicated, and the indanone has a tear gas smell. Therefore, in actual use, it often brings certain inconvenience to users. [0003] Therefore, to provide a preparation method of donepezil hydrochloride with easily available raw materials, simple reaction and safe operation is an urgent problem to be solved by the present invention. Summary of the invention [0004] In view of the above-mentioned prior art, the purpose of the present invention is to overcome the synthesis of donepezil hydrochloride in the prior art by using indano...

Claims

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Application Information

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IPC IPC(8): C07D211/32
CPCC07D211/32
Inventor 王以科
Owner 芜湖耄智生物科技有限公司
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