Method for preparing efletirizine dihydrochloride

A technology of eflurazine hydrochloride and fluorophenyl, which is applied in the field of preparation of eflurazine hydrochloride, can solve the problems of cumbersome steps and low price of raw material compounds, and achieve the effects of simple raw materials, low cost and simple preparation process
CN101928263AInactive Publication Date: 2010-12-29SICHUAN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SICHUAN UNIV
Publication Date
2010-12-29
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for preparing efletirizine dihydrochloride. 1-bis(4-fluoro phenyl)methyl piperazine and an excessive amount of a chloro(ethoxy)acetic acid derivative are heated to condense in a solvent and in the presence of tertiary amine serving as an acid acceptor and alkali halide or halogenated tetrabutyl ammonium serving as a catalyst to form a [2-[4-[bis(fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid derivative; and the [2-[4-[bis(fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid derivative is hydrolyzed and acidized to form the efletirizine dihydrochloride. The method has the advantages of readily available raw materials, simple and convenient operation, high yield and low cost and is suitable for industrial production.
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Description

technical field

[0001] The invention relates to a method for preparing eflurazine hydrochloride, and the compound can treat allergic rhinitis and conjunctivitis. Background technique

[0002] Allergic rhinitis (Allergic Rhinitis), also known as allergic rhinitis, is caused by the body's allergy to certain substances. Its pathogenesis is that allergens cause the body to release histamine, causing a series of allergic symptoms to appear. The clinical features of this disease include nasal itching, continuous sneezing, and a large amount of watery nasal discharge, sometimes accompanied by extreme itching in the conjunctiva, palate, and even the external auditory canal. Due to the swelling of the nasal mucosa, patients often have nasal congestion and hyposmia. Patients usually have no obvious systemic symptoms, but if complicated by sinusitis, they may have symptoms such as fever, cheek distending pain, fatigue and anorexia.

[0003] The treatment principles of this disease a...

Claims

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