Novel preparation process of high-purity escitalopram pamoate

A technology of pamoate and oxalate, applied in the field of chemical medicine, can solve problems such as toxicity

Pending Publication Date: 2020-06-02
SHANGHAI AOBO PHARMTECH INC LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The solvent methanol used in the preparation method of the above-mentioned escitalopram pamoate has certain toxicity

Method used

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  • Novel preparation process of high-purity escitalopram pamoate
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  • Novel preparation process of high-purity escitalopram pamoate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Implementation Example 1: Preparation of Escitalopram Pamoate

[0035] Weigh 500mg of escitalopram oxalate sample, add 25ml of water, and heat to 30°C to dissolve it completely; weigh 520mg of pamoic acid disodium salt, add 12.5ml of water, dissolve it completely at room temperature, and then Add 12.5ml of absolute ethanol and mix well. Add the water / ethanol mixed solution of pamoic acid disodium salt into the escitalopram oxalate aqueous solution dropwise at 30°C, solids appear immediately and the dispersion is good. After the dropwise addition, continue to stir for 2h and then filter. The filter cake was washed with 50ml of water, filtered with suction for 10min, and dried in vacuum. An 850 mg sample of escitalopram pamoate was obtained. Detected by HPLC, the purity is 99.66%

Embodiment 2

[0036] Implementation Example 2: Preparation of Donepezil Pamoate

[0037] Weigh 5g of escitalopram oxalate sample, add 40ml of water, and heat to 60°C to dissolve it completely; weigh 5.2g of pamoic acid disodium salt, add 25ml of water, dissolve it completely at room temperature, and then Add 25ml of absolute ethanol and mix well. Add the water / ethanol mixed solution of pamoic acid disodium salt into the escitalopram oxalate aqueous solution dropwise at 30°C, solids appear immediately and the dispersion is good. After the dropwise addition, continue to stir for 2h and then filter. The filter cake was washed with 50ml of water, filtered with suction for 10min, and dried in vacuum. An 8.5 g sample of escitalopram pamoate was obtained. As detected by HPLC, the purity was 99.71%.

Embodiment 3

[0038] Implementation Example 3: Preparation of Donepezil Pamoate

[0039] Weigh 50g of escitalopram oxalate sample, add 400ml of water, heat to 60°C to dissolve it completely; weigh 52g of pamoic acid disodium salt, add 250ml of water, dissolve it completely at room temperature, then add 250ml absolute ethanol, mix well. Add the water / ethanol mixed solution of pamoic acid disodium salt into the escitalopram oxalate aqueous solution dropwise at 30°C, solids appear immediately and the dispersion is good. After the dropwise addition, continue to stir for 2h and then filter. The filter cake was washed with 500ml of water, filtered with suction for 10min, and dried in vacuum. An 85 g sample of escitalopram pamoate was obtained. As detected by HPLC, the purity was 99.70%.

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Abstract

The invention relates to a novel preparation method of escitalopram pamoate ((S)-(+)-1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydro-5-cyano isobenzofuran pamoate), wherein the method is environment-friendly and pollution-free, and escitalopram pamoate prepared by the method is high in purity and good in repeatability.

Description

technical field [0001] Escitalopram pamoate ((S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro The invention discloses a new preparation method of 5-cyanoisobenzofuran pamoate, which belongs to the field of chemical medicine. [0002] technical background [0003] Escitalopram, chemical name: (S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-di Hydrogen-5 cyanoisobenzofuran. Escitalopram oxalate was jointly developed by Forest Laboratories of the United States and Lundbeck of Denmark. It was first launched in Switzerland and other European and American countries in March 2002, and was approved by the FDA in August. Escitalopram is a serotonin reuptake inhibitor (SSRI), which has a unique serotonin isomeric site binding mechanism and is highly selective for serotonin receptors. It is used for the treatment of major depression and Maintenance treatment of depression. [0004] Patients with major depression are often non-compliant, making it difficu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/87
CPCC07D307/87C07B2200/13
Inventor 许炜陈茜顾虹
Owner SHANGHAI AOBO PHARMTECH INC LTD
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