Preparation method of nalmefene hydrochloride monohydrate

A technology of nalmefene hydrochloride and monohydrate, which is applied in the field of preparation of nalmefene hydrochloride monohydrate, can solve the problems of poor stability and low yield of nalmefene hydrochloride monohydrate, and achieve good stability and improved Yield effect

Active Publication Date: 2016-06-08
南京卓康医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] CN102325778A discloses the preparation method of nalmefene hydrochloride monohydrate, but the prepared nalmefene hydrochloride monohydrate has low yield, poor stability and hygroscopicity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] 5.0g nalmefene hydrochloride sample (moisture content 3.57%) was dispersed with 50ml dichloromethane, slowly dripped into 2.4g purified water under stirring, heated to reflux for 1h, then cooled to 10-15°C for filtration, and the filter cake was dried at 40°C to Constant weight was obtained to obtain nalmefene hydrochloride monohydrate, the yield was 4.68g, the water content was 5.23%, and the yield was 92.0%.

Embodiment 2

[0016] 5.0g nalmefene hydrochloride sample (moisture content 3.57%) was dispersed in 50ml dichloromethane, slowly dripped into 1.2g purified water under stirring, heated to reflux for 1h, then cooled to 10-15°C for filtration, and the filter cake was dried at 40°C to Constant weight was obtained to obtain nalmefene hydrochloride monohydrate, the yield was 4.66g, the water content was 5.11%, and the yield was 91.7%.

Embodiment 3

[0018] 5.0g nalmefene hydrochloride sample (moisture content 3.57%) was dispersed in 50ml dichloromethane, slowly dripped into 3.6g purified water under stirring, heated to reflux for 1h, then cooled to 10-15°C for filtration, and the filter cake was dried at 40°C to Constant weight was obtained to obtain nalmefene hydrochloride monohydrate, the yield was 4.48g, the water content was 5.25%, and the yield was 88.0%.

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Abstract

The invention discloses a preparation method of a nalmefene hydrochloride monohydrate. According to the method, nalmefene hydrochloride is dispersed in a specific organic solvent, water is added, the dosage is controlled, and crystal transformation is performed. The prepared nalmefene hydrochloride monohydrate has the advantages of high yield, high purity, high stability and good nonabsorbent property.

Description

technical field [0001] The invention relates to a preparation method of nalmefene hydrochloride monohydrate. Background technique [0002] Nalmefene is a known opioid receptor antagonist that inhibits the pharmacologic effects of both administered opioid agonists and agonists endogenously produced by the opioid system. The clinical effectiveness of nalmefene as an antagonist stems from its ability to rapidly (and selectively) reverse the effects of these opioid agonists, including common depression in the central nervous system and respiratory system. Nalmefene is an opiate derivative structurally similar to the opiate antagonist naltrexone. Advantages of nalmefene over naltrexone include a longer half-life, greater oral bioavailability, and no dose-dependent hepatotoxicity observed. [0003] CN102325778A discloses a preparation method of nalmefene hydrochloride monohydrate, but the prepared nalmefene hydrochloride monohydrate has low yield, poor stability and hygroscopici...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D489/08
CPCC07D489/08
Inventor 吴庆波李强
Owner 南京卓康医药科技有限公司
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