Aryl piperazine modified benzo [b] thiophene compounds and their preparation method and use

An arylpiperazine and compound technology, applied in the field of medicinal chemistry, can solve the problems of lag effect, nausea, anxiety, insomnia, research urgency, etc., and achieve the effects of easy operation and simple preparation process
CN1844120AInactive Publication Date: 2006-10-11TIANJIN UNIV

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
TIANJIN UNIV
Publication Date
2006-10-11
Estimated Expiration
Not applicable · inactive patent

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Abstract

This invention belongin to medicinal chemistry, pubilize the structure and synthesis of aryl-diethylenediamine modified benzo[b]thiophenes with antidepressant function. Its structure is depicted as picuture. Ar structure is as depicted.the synthesis of the compound is as followings: mix 1M 3-propionyl benzo[b]thiophenes,1-5M cavaform and 1-5M aryl-piperazidine hydrochlorate in 1-50 weight folds ethanol, inverse flowing react 1-80 hours, obtain 1-( benzo[b]thiophenes-3)-2- methyl-3-( 4-aryl-piperazidine-)1- acetone; Mix 1M 1-( benzo[b]thiophenes-3)-2- methyl-3-( 4-aryl-piperazidine-)1- acetone and 0.2-5M sodium borohydride in 1-50 weight folds of ethanol, react at 0-100deg C for 1-20, 1-( benzo[b]thiophenes-3)-2- methyl-3-( 4-aryl-piperazidine-)1- propanol obtained. This kind of compounds could be used for antidepressant drug preparation in the form of free alkali or salt. This invention is advantageous in simplied preparation and easy manipulation.
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Description

technical field

[0001] The invention relates to the structure, preparation method and application of an arylpiperazine-modified benzo[b]thiophene compound with antidepressant activity, and belongs to the field of medicinal chemistry. Background technique

[0002] Depression is a common mental illness, which is an emotional disorder. As the pace of life continues to accelerate, people's mental pressure is gradually increasing. Depression has become a common disease in modern society, with a high incidence, and its incidence is rising rapidly. : According to incomplete statistics, at present the world's depression patients have accounted for 3%-5% of the world's population, almost seen in all ages, and its prevalence is about 3% in the general population, and the patient population in general hospital health services In patients with chronic physical diseases (such as cardiovascular disease, diabetes), the rate of depressive disorder can be as high as 20%, but only a very smal...

Claims

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