Preparation method of 5-(piperazine-1-group) benzofuran-2-carboxylic acid ethyl ester

A technology of benzofuran and ethyl carboxylate, which is applied in the field of preparation of ethyl 5-benzofuran-2-carboxylate, can solve the problems of low yield, no post-treatment method and yield given, and achieve The effect of improving yield and product purity, simple and reliable method, and shortening reaction time
CN102633759AInactive Publication Date: 2012-08-15SHANDONG ZOUPING DAZHAN NEW MATERIALS
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG ZOUPING DAZHAN NEW MATERIALS
Publication Date
2012-08-15
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a preparation method of 5-(piperazine-1-group) benzofuran-2-carboxylic acid ethyl ester. 5-(piperazine-1-group) benzofuran-2-carboxylic acid ethyl ester is an important intermediate for synthetizing hydrochloric vilazodone. Under the existence of alkali and phase transfer catalyst, 5-amino-benzofuran-2-carboxylic acid ethyl ester and N, N-di (2-chlorine ethyl) amine hydrochloride are reacted in solvent, reaction time is 2-6 hours, and reaction temperature ranges from room temperature to backflow temperature of the solvent. By the preparation method, reaction time is shortened, and yield rate and purity of products are improved. The preparation method is simple, reliable and low in production cost and has higher implement value and social and economic benefits.
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Description

technical field

[0001] The invention relates to a preparation method of ethyl 5-(piperazin-1-yl)benzofuran-2-carboxylate, which is an important intermediate for synthesizing vilazodone hydrochloride. Background technique

[0002] Vilazodone hydrochloride was approved by the US Food and Drug Administration in January 2011 for the treatment of moderate to severe depression in adults. Clinical trial data show that its curative effect is significantly better than that of placebo, with good tolerance and less adverse reactions.

[0003] 5-(piperazin-1-yl) ethyl benzofuran-2-carboxylate is the key intermediate of synthetic vilazodone hydrochloride, and a kind of its synthetic method is announced in U.S. Patent No. 5,723,614 as follows:

[0004]

[0005] In this method, ethyl 5-aminobenzofuran-2-carboxylate is used as raw material and N,N-bis(2-chloroethyl)amine to react with stirring for 10 hours to prepare 5-(piperazin-1-yl)benzo Ethyl furan-2-carboxylate, but did not give a...

Claims

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