Benzoyl-containing rupestonic acid methyl ester derivative as well as preparation method and application thereof

The invention relates to a benzoyl-containing rupestonic acid methyl ester derivative as well as a preparation method and application thereof. Rupestonic acid and dimethyl sulfate react to obtain rupestonic acid methyl ester, 2-hydroxyl rupestonic acid methyl ester is prepared under oxidation of cam...

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Hauptverfasser: CHEN LEI, AJIAIKEBAIER AISA, ZHAO JIANGYU
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AJIAIKEBAIER AISA
ZHAO JIANGYU
description The invention relates to a benzoyl-containing rupestonic acid methyl ester derivative as well as a preparation method and application thereof. Rupestonic acid and dimethyl sulfate react to obtain rupestonic acid methyl ester, 2-hydroxyl rupestonic acid methyl ester is prepared under oxidation of camphor sulfonyl acridine, and then the 2-hydroxyl rupestonic acid methyl ester reacts with different substituted benzoyl chloride under the catalysis of DMAP to obtain the 1d-15d benzoyl-containing rupestonic acid methyl ester derivative. The method has the advantages of mild reaction conditions and simple experimental steps. The obtained benzoyl-containing rupestonic acid methyl ester derivative 1d-15d is subjected to an anti-H3N2 influenza A virus activity test in 1d-15d. Experimental results show that the compounds 1d, 2d, 4d, 5d, 7d, 8d, 12d, 13d and 15d can be applied to preparation of drugs for resisting influenza A H3N2 virus. 本发明涉及一种含苯甲酰基的一枝蒿酮酸甲酯衍生物及其制备方法和用途,该类衍生物是由一枝蒿酮酸和硫酸二甲酯反应得到一枝蒿酮酸甲酯,在樟脑磺酰吖啶的氧化下制备得到2-羟基一枝
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Rupestonic acid and dimethyl sulfate react to obtain rupestonic acid methyl ester, 2-hydroxyl rupestonic acid methyl ester is prepared under oxidation of camphor sulfonyl acridine, and then the 2-hydroxyl rupestonic acid methyl ester reacts with different substituted benzoyl chloride under the catalysis of DMAP to obtain the 1d-15d benzoyl-containing rupestonic acid methyl ester derivative. The method has the advantages of mild reaction conditions and simple experimental steps. The obtained benzoyl-containing rupestonic acid methyl ester derivative 1d-15d is subjected to an anti-H3N2 influenza A virus activity test in 1d-15d. 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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Benzoyl-containing rupestonic acid methyl ester derivative as well as preparation method and application thereof
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