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
CN1726202AInactive Publication Date: 2006-01-25H LUNDBECK AS
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
H LUNDBECK AS
Publication Date
2006-01-25
Estimated Expiration
Not applicable · inactive patent

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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.
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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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