Substituted benzene propenyl piperazinyl alkyl polyhydric benzamide compound and preparation method and application thereof

A compound and alkyl technology, which is applied in the field of preparation of HIV-1 integrase inhibitors, can solve the problems of drug resistance, central nervous disorder, multi-drug resistance, etc., and achieve the effect of mild reaction conditions and simple steps
CN101665473BInactive Publication Date: 2011-05-11BEIJING UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Patents(China)
Current Assignee / Owner
BEIJING UNIV OF TECH
Publication Date
2011-05-11
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The invention relates to a (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl benzamide compound shown in a formula (I) or a salt thereof, wherein R<1>, R<2> and R<3> express -H, -OH, -ONa, -OK or -ONH4, R<4> and R<5> express-H, halogen, C(1-3) linear or branched alkyl, -OH, -ONa, -OK, -ONH4, -NO2 or -CN, and n is an integer of 1-3. The invention also relates to a preparation methodof the compound, which comprises the following steps: synthesizing multi-alkoxy benzoyl chloride substituted alkylamine by using multi-substituted benzoyl chloride and hydrochloride of chlorinated alkyl amino as raw materials; carrying out reaction on the compound and piperazine to prepare N-piperazinyl alkyl multi-substituted benzamide; reacting with substituted benzene acryloyl chloride to prepare (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl benzamide; acting with BBr3 or BF3 aether solution to be further hydrolyzed to generate the corresponding (E)-N-3-(4-substituted benzene propenyl piperazine-1-base) alkyl polyhydric benzamide compound, and then reacting with alkaline to generate the corresponding salt. The compound has inhibition function to HIV-1 integrase.
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Description

technical field

[0001] The invention relates to (E)-N-3-(4-substituted phenylpropenylpiperazin-1-yl)alkylbenzamide compounds and their salts, their preparation methods and their use in the preparation of HIV-1 integrase inhibitors in the application. Background technique

[0002] AIDS is a major infectious disease that gradually destroys the human immune system and seriously threatens human health and survival. Since it was first discovered in 1981, it has spread rapidly around the world. By the end of 2008, there were 33.2 million surviving HIV-1 infections worldwide. In 2008, there were 2.5 million new infections and 2.1 million deaths. 70 million people.

[0003] HIV-1 (Human Immunodeficiency Virus-I), which belongs to retroviruses, is a virus that causes AIDS (Acquired Immunodeficiency Syndrome, AIDS).

[0004] HIV-1 targets CD4-positive cell populations such as helper T cells, macrophages, and dendritic cells, etc., and destroys these immunocompetent cells, resulting...

Claims

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