Coffee acyl naphthalene sulfonamides compound and method for preparing the same and anti HIV conformity enzyme action

A technology of naphthalenesulfonamide and caffeamide, which is applied in the field of caffeoylnaphthalenesulfonamide compounds and their preparation, and achieves the effects of simple preparation method, favorable industrial production and high yield
CN1482116AInactive Publication Date: 2004-03-17QINGDAO HUANGHAI PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
QINGDAO HUANGHAI PHARM CO LTD
Publication Date
2004-03-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention relates to caffeoyl naphthalene sulfamide compound. The compound is prepared with 5-acetamido-1-sodium naphthalenesulfonate as material and through reaction first with chlorosulfonic acid and then with amine compound to obtain 5-(N-substituted amino)-sulfonyl-1-naphthylamine; reaction with 3, 4-diacetylcaffeoyl chloride to obtain N-[[5-[(N-substrate)-amino]-sulfonyl]-1-naphthyl]-3, 4-diacetylcaffeoylamine; and hydrolysis to obtain N-[[5-[(N-substrate)-amino]-sulfonyl]-1-naphthyl]-caffeoylamine. The present invention also relates to the application of the compound as human immune deficiency virus integrase inhibitor.
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Description

(1) Technical field

[0001] The invention relates to caffeamide compounds and their synthesis, preparation methods and applications, in particular to caffeoylnaphthalenesulfonamide compounds, their preparation methods and their anti-HIV integrase effects. (2) Background technology

[0002] Human immunodeficiency virus (Human immunodeficiency virus, HIV) is the pathogenic factor of AIDS (Acquiredimmuneficiency syndrome, AIDS). HIV is a single-strand ribonucleic acid (RNA) virus, and reverse transcriptase (Reverse transcriptase), protease (Protease) and integrase (Integrase) are three key enzymes in the process of HIV replication. Currently, only reverse transcriptase inhibitors and protease inhibitors are currently used in the clinical treatment of AIDS. For patients who have been treated with reverse transcriptase and protease inhibitors alone or in combination, the serum new viral load rebounds rapidly after stopping the drug, and most of the patients who have undergone che...

Claims

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