Benzimidazole derivative and preparation method and application thereof

A technology of benzimidazoles and benzimidazoles, which is applied in the field of benzimidazole derivatives and their preparation, can solve the problems of lack of anti-drug addiction compounds and can only take medicines for life, etc., and achieves wide practicability and development value , reducing the relapse rate and suppressing the effects of morphine withdrawal symptoms

Inactive Publication Date: 2018-12-14
TIBET UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the benzimidazole derivatives disclosed in journals and patent documents are mainly used in various diseases such as tumors, and no benzimidazole derivatives that can be used to resist drug addiction have been disclosed or researched. The commonly used treatment method for psychological craving after drug dependence withdrawal is substitution therapy. The psychological craving is still difficult to eliminate and can only be taken for life. At present, there is an extreme lack of effective anti-drug addiction compounds. Therefore, the research and development of effective drug addiction psychological The desired compound is imminent

Method used

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  • Benzimidazole derivative and preparation method and application thereof
  • Benzimidazole derivative and preparation method and application thereof
  • Benzimidazole derivative and preparation method and application thereof

Examples

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Embodiment 1

[0037] Embodiment 1: A kind of benzimidazole derivative

[0038] The present invention specifically provides a benzimidazole derivative represented by general formula (I):

[0039]

[0040] Preferably, in general formula (I), R 1 =H.

[0041] Preferably, in general formula (I), R 2 =H or O.

[0042] Preferably, in the general formula (I), X═C or N or O or S.

[0043] Preferably, in the general formula (I), n=0 or 1.

[0044] Preferably, in general formula (I), R 1 It is any one of an alkyl substituent, a phenyl substituent, and a benzyl substituent.

[0045] Preferably, in general formula (I), R 2 Any of an alkyl substituent, a phenyl substituent, a benzyl substituent, and an acyl substituent.

Embodiment 2

[0046] Embodiment two: the preparation method of benzimidazole derivatives

[0047] Specifically adopt the following steps to prepare benzimidazole derivatives:

[0048]

Embodiment 3

[0049] Example 3: Preparation and structure identification of benzimidazole derivative TUP-01

[0050]Take a 30mL dried microwave tube, add 2-chlorobenzimidazole (0.457g, 3mmol), dissolve in 6mL of methanol, add tetrahydropyrrole (0.32mL, 3.9mmol), and react in microwave at 160°C for 2.5h. Spin to dry the solvent, add 200mL ethyl acetate to dissolve, wash with 200mL water and 200mL saturated brine respectively, and dry the organic phase with anhydrous sodium sulfate. The organic phase was spin-dried to obtain the benzimidazole derivative TUP-01, 0.274 g of white solid, with a yield of 41%. The structural formula of benzimidazole derivative TUP-01 is:

[0051]

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Abstract

The invention discloses a benzimidazole derivative and a preparation method and the application thereof. The prepared benzimidazole derivative is capable of effectively reducing the relapse arte afterabstaining from morphine addiction, has a remarkable effect for restraining morphine abstaining symptoms, has wide practicability in the technical field of preparing drugs for preventing and / or treating drug addiction, and has a relatively high value in the technical field of preparing drugs for preventing and / or treating relapse after dependence producing drug abstaining.

Description

technical field [0001] The present invention mainly relates to the technical field of pharmaceutical chemical preparation, in particular, the present invention relates to the technical field of benzimidazole derivatives and their preparation methods and applications. Background technique [0002] Drug addiction is a chronic recurrent brain disease characterized by compulsive drug use and loss of control. Relapse is a difficult part of detoxification treatment. The international anti-drug convention divides the drugs of dependence into three categories: narcotic drugs, psychotropic drugs and others. Among them, narcotic drugs are divided into opioids, cocaine, cannabis, etc.; psychotropic drugs are divided into sedative hypnotics and anxiolytics such as barbiturates, central stimulants such as amphetamines, hallucinogens such as ergot diethylamine, etc.; It also includes alcohol, tobacco and volatile organic solvents. Drug addiction has become a worldwide public health and...

Claims

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Application Information

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IPC IPC(8): C07D401/04C07D235/30C07D491/113C07D401/14A61P25/34A61P25/32A61P25/36A61P25/30
CPCA61P25/30A61P25/32A61P25/34A61P25/36C07D235/30C07D401/04C07D401/14C07D491/113
Inventor 徐福春洪学传田甜李艳琴列谢
Owner TIBET UNIV
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