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Production process of paroxetine hydrochloride

A paroxetine hydrochloride and production process technology, applied in the field of paroxetine hydrochloride production process, can solve the problems of low yield of paroxetine hydrochloride, incomplete reaction of N-methyl paroxetine, etc., to ensure stable quality and safety control, Improvement of yield and purity, effect of improving yield and purity

Inactive Publication Date: 2015-03-25
CHENGDU YILUKANG MEDICAL TECH & SERVICE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The main purpose of the present invention is to provide a new production process with high yield of paroxetine hydrochloride for the incomplete reaction of N-methylparoxetine in the prior art, which leads to low yield of paroxetine hydrochloride

Method used

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  • Production process of paroxetine hydrochloride
  • Production process of paroxetine hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Add 20 g of N-methylparoxetine and 200 ml of toluene into the three-necked flask, slowly add a mixture of 9.4 g of vinyl chloroformate and 20 ml of toluene dropwise at room temperature, and react at 80° C. for 6 hours after dropping by TLC (dichloromethane:methanol= 5:1) Monitor until the reaction is complete, add 200ml of water to the reaction solution, stir, separate layers, keep the organic layer, extract the water layer once with 100ml toluene, combine the organic layers, and wash three times with 200ml water respectively. The organic layer was concentrated under reduced pressure to obtain 22.2 g of oily substance, with a yield of 95%.

Embodiment 2

[0023] Add 20 g of the oil obtained in Example 1, 200 ml of toluene, and 6 g of potassium hydroxide to a three-neck flask, and react at 80° C. for 24 hours. TLC monitors until the reaction is complete (dichloromethane: ethyl acetate = 5:1), add water to separate layers , collect the organic layer, extract the water layer once with 100ml toluene, combine the organic layers, wash three times with 200ml respectively, take the organic layer and add concentrated hydrochloric acid under stirring, a large amount of light yellow crystals are precipitated, suction filtered and dried to obtain the crude product of light yellow paroxetine hydrochloride 18g, yield 95%.

Embodiment 3

[0025] Add 18 g of the crude product of paroxetine hydrochloride into the three-necked flask, and add 180 ml of acetone. Raise the temperature to 66°C, add 2% activated carbon, and reflux for 30 minutes to decolorize. Suction filtration, stirring the filtrate to cool down to 0°C, suction filtration and drying to obtain 16.5 g of finished paroxetine hydrochloride.

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Abstract

The invention discloses a production process of paroxetine hydrochloride and belongs to the technical field of medicines. The compound paroxetine hydrochloride has the following structure as shown in the specification. According to the invention, the demethylation reaction of N-methyl paroxetine is mainly studied in detail and the refining process of paroxetine hydrochloride is relevantly inspected. Industrially available vinyl chloroformate is adopted as a demethylation reagent, reaction conditions are mild and the total yield is above 90%. By adopting acetone of which the use amount is 10 times amount of a paroxetine hydrochloride crude product as a refining solvent, a majority of impurities can be well removed to obtain pure white crystalline powder of which the content is above 99.8%.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a production process of paroxetine hydrochloride. Background technique [0002] Paroxetine, (-)-trans-4-(4-fluorophenyl)-3-[[3,4-(methylenedioxy)phenoxy]methyl]-piperidine. This product is a selective 5-HT reuptake inhibitor, and it has no obvious effect on other transmitters at the usual dose. It increases the concentration of 5-HT in the synaptic cleft by preventing the reabsorption of 5-HT, thereby producing an antidepressant effect. Paroxetine exerts its drug effect by inhibiting the reuptake of 5-TH in brain neurons, and its selectivity is stronger than that of fluoxetine, sertraline or clomipramine. Low affinity for cholinergic, histamine or adrenergic receptors, less anticholinergic and cardiovascular side effects than tricyclic antidepressants. There were no cognitive or psychomotor impairments. Hematological, biochemical, and urological parameters were not specifica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12
CPCC07D405/12
Inventor 彭超
Owner CHENGDU YILUKANG MEDICAL TECH & SERVICE
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