Agomelatine sulfate and preparation method thereof

A technology of agomelatine and sulfate, applied in the field of agomelatine sulfate and preparation thereof, can solve the problems of lack of purity and high agomelatine sulfate, and achieve good fluidity , Improve the purity, good crystallization effect

Active Publication Date: 2012-10-10
FUJIAN COSUNTER PHARMA
View PDF4 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Agomelatine can be mixed with many acids to form complexes with stable physical and chemical properties. For example, the Shanghai Pharmaceutical Industry Research Institute has made complexes

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Agomelatine sulfate and preparation method thereof
  • Agomelatine sulfate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Take 2 grams of agomelatine crude product with a purity of 95.8%, stir and dissolve it with 20 ml of anhydrous ethyl acetate, and slowly add 0.5 ml of concentrated sulfuric acid dropwise in a water bath at room temperature, and a large amount of white solids will precipitate out. Stir for another hour, filter, wash with a small amount of ethyl acetate, and dry at 60°C to obtain 2.7 g of a white solid with a yield of 96.2%, a purity of >99.5%, and a melting point of 160-163°C.

Embodiment 2

[0036] Take 4 grams of agomelatine crude product with a purity of 95.8%, stir and dissolve it with 40 ml of anhydrous ethyl acetate, slowly add 1 ml of concentrated sulfuric acid dropwise in a water bath at room temperature, and a large amount of white solids will precipitate out. Stir for another hour, filter, wash with a small amount of ethyl acetate, and dry at 60°C to obtain 5.48 g of a white solid with a yield of 97.6%, a purity of >99.5%, and a melting point of 160-163°C.

Embodiment 3

[0038] Take 4 grams of agomelatine crude product with a purity of 99.1%, stir and dissolve it with 40 ml of anhydrous ethyl acetate, slowly add 1 ml of concentrated sulfuric acid dropwise in a water bath at room temperature, and a large amount of white solids will precipitate out. Stir for another hour, filter, wash with a small amount of ethyl acetate, and dry at 60°C to obtain 5.5 g of a white solid with a yield of 98.0%, a purity of >99.6%, and a melting point of 160-163°C.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Melting pointaaaaaaaaaa
Login to view more

Abstract

The invention relates to agomelatine sulfate and a preparation method thereof. An unexpected discovery is that the solubility and stability of agomelatine can be improved when agomelatine is prepared into sulfate, and production of appropriate pharmaceutical preparations with agomelatine can be facilitated. In the preparation method, the agomelatine sulfate is prepared via reaction of agomelatine and sulfuric acid. The preparation method specifically comprises the steps of: dissolving agomelatine in an organic solvent, slowly adding concentrated sulfuric acid at normal temperature, precipitating a large amount of solid until the raw material agomelatine disappear according to TLC (thin-Layer chromatography) tracking results, filtering, washing and drying the solution , thereby obtaining the target product.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to agomelatine sulfate and a preparation method thereof. Background technique [0002] The chemical name of agomelatine is N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, and its structural formula is shown in the following formula (II). Its trade name is Valdoxan, which is the first melatonin antidepressant developed by Servier in France, and it was launched in Germany and the United Kingdom in 2009. It can effectively treat depression, improve sleep parameters and maintain sleep quality. features of sexual function. [0003] [0004] Agomelatine has dual properties. On the one hand, it is an agonist of the melatonin receptor; on the other hand, it is an antagonist of the 5-HT2C receptor. These properties make it central nervous system active, especially in the treatment of major depression, seasonal affective disorder, sleep disorders, cardiovascular conditions, digestive system conditions,...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07C233/18A61K31/165A61P25/24A61P25/20A61P25/18A61P9/00A61P1/00A61P39/00A61P3/04C07C231/12
Inventor 姚建堤陈首鹤陈仕魁杨喜鸿苏葳
Owner FUJIAN COSUNTER PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap