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Continuous preparation method of paroxetine hydrochloride

A technology of paroxetine hydrochloride and paroxol, which is applied in the field of medicine, can solve the problems of being unsuitable for continuous chemical industrial production, unfavorable environmental protection, and high price, and achieves the control of the generation of toxic impurities, which is beneficial to environmental protection and has fewer purification steps Effect

Pending Publication Date: 2021-03-19
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The preparation method of existing multiple paroxetine hydrochloride is reported in the prior art, for example CN104447714A and CN102718756A, it all uses N-methyl paroxetine as raw material, and this raw material price is higher, is not suitable as the starting point of producing paroxetine hydrochloride raw material
In addition, the intermediate product of the above-mentioned patented paroxetine hydrochloride preparation method needs to undergo purification operations such as liquid separation, extraction, washing, and concentration under reduced pressure. Continuous chemical industry production, production efficiency is low; In addition, the preparation method of above-mentioned paroxetine hydrochloride also can produce a large amount of waste liquids because a large amount of use solvents, is unfavorable for the requirement of environmental protection

Method used

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  • Continuous preparation method of paroxetine hydrochloride
  • Continuous preparation method of paroxetine hydrochloride
  • Continuous preparation method of paroxetine hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Preparation of Paroxetine Hydrochloride Crude Product

[0033] 1) Add 500kg of toluene, 50kg of trans-parol, and 60kg of p-toluenesulfonyl chloride into a 1000L glass-lined reactor, stir and cool down to -5~5°C, and add 32kg of triethylamine to control the temperature at -5~5°C. Raise the temperature to 25°C and react for 4 hours. TLC monitors that the reaction is complete, and the reaction solution is transferred to a 1000L stainless steel reactor for later use;

[0034] 2) Add 100 kg of 20% aqueous sodium hydroxide solution to the above-mentioned stainless steel reaction kettle, stir for 1 hour, let stand, separate liquids, leave the organic phase in the stainless steel reaction kettle, add 3 kg of tetrabutylammonium bromide, sesame seeds to the stainless steel reaction kettle 34kg of phenol, stirred evenly, added 150kg of 40% sodium hydroxide aqueous solution, heated to reflux for 2 hours, TLC monitored the reaction to be complete, cooled to room temperature, all...

Embodiment 2

[0040] 1) Preparation of Paroxetine Hydrochloride Crude Product

[0041] 1) Add 550kg of xylene, 50kg of trans-parol, and 51.2kg of p-toluenesulfonyl chloride into a 1000L glass-lined reactor, stir and cool down to -5~5°C, and add 16.4kg of ethanolamine to control the temperature at -5~5°C , the temperature was raised to -5°C for 8 hours, the reaction was monitored by TLC, and the reaction solution was transferred to a 1000L stainless steel reactor for later use;

[0042] 2) Add 100kg of 20% aqueous sodium hydroxide solution in the above-mentioned stainless steel reaction kettle, stir for 1 hour, leave standstill, separate liquids, the organic phase stays in the stainless steel reaction kettle, add tetrabutylammonium chloride 1.9kg, Sesamol 30.9kg, stir evenly, add 112kg of 40% sodium hydroxide aqueous solution, heat up to reflux reaction for 2 hours, TLC monitors that the reaction is complete, cool down to room temperature, let stand, separate liquids, and transfer the organic ...

Embodiment 3

[0048] (1) Preparation of Paroxetine Hydrochloride Crude Product

[0049] 1) Add 500kg of cyclohexane, 50kg of trans-parol, and 64.0kg of p-toluenesulfonyl chloride into a 1000L titanium reactor, stir and cool down to -5~5°C, control the temperature at -5~5°C and add sodium bicarbonate 33.9kg, heated up to 30°C for 3 hours, TLC monitored the reaction was complete;

[0050] 2) Add 100 kg of 20% aqueous sodium hydroxide solution to the above-mentioned titanium reactor, stir for 1 hour, let stand and separate liquids, leave the organic phase in the titanium reactor, and add 7.2 kg of tetrabutylammonium bromide to the titanium reactor 1. Sesamol 46.4kg, stir evenly, add 448kg of 40% aqueous sodium hydroxide solution, heat up to reflux reaction for 2 hours, TLC monitors that the reaction is complete, cool down to room temperature, leave standstill, separate liquid, and the organic phase is retained in the titanium reactor;

[0051] 3) Heat the titanium reactor containing the organ...

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Abstract

The invention relates to a continuous preparation method of paroxetine hydrochloride, which is characterized in that trans-paroxetine and sesamol are taken as raw materials, paroxetine hydrochloride is obtained through four steps, the purification steps of an intermediate in the reaction process are few, the intermediate and a solvent can directly enter the next step for reaction, and by controlling the reaction conditions, the paroxetine hydrochloride product is directly obtained. The whole production process has the advantages of less generation of three wastes, low cost and few treatment procedures.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a continuous preparation method of paroxetine hydrochloride. Background technique [0002] Depression is recognized by the medical community as a common mental illness. About 350 million people around the world suffer from depression to varying degrees, accounting for about 4.4% of the total global population. About 55 million people in my country suffer from depression, and about 1 million people commit suicide every year due to depression. In view of the increasing trend of the incidence of depression and its harm to society, medical workers continue to develop new antidepressant drugs. According to the different mechanisms of action, currently commonly used antidepressants can be simply divided into four categories: monoamine oxidase inhibitors (MAOIs), tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs), Serotonin and norepinephrin...

Claims

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Application Information

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IPC IPC(8): C07D405/12
CPCC07D405/12
Inventor 马德彪刘志东徐晓东王旭进任富兴张高亮杜秋张松刘丙乾周世利
Owner BEIJING WINSUNNY PHARMA CO LTD
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