(Z)-1-(1-substituted benzyl-5-methyl-1H-1,2,3-triazole-4-yl)-3-substituted benzyl-3-hydroxy-2-propylene-1-ketone compound and preparation method and application thereof

A compound, benzyl technology, applied in the field of HIV integrase inhibitors, can solve the problem of easy reduction of enol, and achieve the effect of mild reaction conditions

CN102503900AInactive Publication Date: 2012-06-20BEIJING UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
Publication Date
2012-06-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to (Z)-1-(1-substituted benzyl-5-methyl-1H-1,2,3-triazole-4-yl)-3-substituted benzyl-3-hydroxy-2-propylene-1-ketone compound and a preparation method and an application thereof. The compound is expressed by formula (I), wherein R1 represents -F, R2 represents -H, or R1 represents -H, R2 represents -F; R3, R4 and R5 represent -OH or -H. The preparation method of the compound comprises synthesizing fluoro-benzyl azide with mono-fluoro benzyl bromide as raw material, reacting with acetylacetone to obtain 1-(1-fluoro-benzyl)-4-acetyl-5-methyl)-1H-1,2,3-triazole, carrying out condensation reaction with substituted methyl benzoate to obtain a compound having a dicarboxylic acid structure, and finally demethylating with boron tribromide to obtain the compound. The compound provided by the invention has an inhibitory action to HIV-1 (human immunodeficiency virus-1) integrase.
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