Crystalline escitalopram hydrobromide and methods for preparing the same

A technology of escitalopram and hydrobromide, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, digestive system, etc., and can solve problems such as failure to achieve success

Inactive Publication Date: 2006-01-25
H LUNDBECK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Crystalline salts with hydrochloric and hydrobromic acids have so far been unsuccessful

Method used

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  • Crystalline escitalopram hydrobromide and methods for preparing the same
  • Crystalline escitalopram hydrobromide and methods for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0026] A) Experiment with HCl gas: A 250 ml round bottom flask was charged with 5.7 g of escitalopram free base and 120 ml of isopropanol. The mixture was stirred until a homogeneous solution was obtained. The mixture was cooled to 5 °C and HCl gas was bubbled through for 20 minutes with cooling. The mixture is kept in the refrigerator overnight. No solid material formed. The mixture was then concentrated in vacuo to an oil, and the oily residue was dissolved in acetone (solution was 0.5 molar in acetone) by heating to 45°C. The flask was scraped to start nucleation and the solution became cloudy. The solution was cooled to 5°C overnight. The fluffy material was collected by filtration, transferred to a tan bottle and dried (50°C HI-VAC) to a powder. A sample of this powder is exposed to air, and when it absorbs moisture from the air, it turns into an oil. Recrystallization of the oil was attempted using various solvents. However, none of these trials resulted in a soli...

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PUM

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Abstract

The present invention provides an escitalopram (S-citalopram) in the form of its hydrobromide, methods for the preparation thereof and pharmaceutical compositions thereof.

Description

[0001] The present invention relates to escitalopram in the hydrobromide form, which is the S-enantiomer of the known antidepressant citalopram, i.e. (S)-1-[3-(dimethylamino)propyl]- 1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuronitrile, and a method for its preparation. Background of the invention [0002] Citalopram is a well known antidepressant that has been on the market for many years and has the following structure: [0003] [0004] It is a selective, centrally acting serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitor with corresponding antidepressant activity. Citalopram was first disclosed in DE 2,657,013 (equivalent to US 4,136,193). [0005] Diol, 4-[4-(dimethylamino)-1-(4'-fluorophenyl)-1-hydroxy-1-butyl]-3-(hydroxymethyl)-benzonitrile, and its preparation as The use of intermediates of citalopram has been disclosed, for example, in US Pat. No. 4,650,884. [0006] S-enantiomer of formula (escitalopram) [0007] [0008] and the antidepressant effect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/87A61K31/343A61P25/00A61P25/22A61P25/24A61P25/30
CPCA61K31/343C07D307/87A61P1/14A61P15/00A61P25/00A61P25/14A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P25/36A61P3/04
Inventor L·马特尔R·丹塞尔H·彼得森P·埃勒加德
Owner H LUNDBECK AS
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