合成新型 4-烷基-6-（5-芳基-1,2,3-噻二唑-4-基）苯-1,3-二醇作为潜在的 Hsp90 抑制剂

IF 0.5 4区化学 Q4 CHEMISTRY, MULTIDISCIPLINARY

Chemija Pub Date : 2023-12-07 DOI:10.6001/chemija.2023.34.4.2

Paulina Kaziukonytė, Tomas Venslauskas, Kamilė Venskūnaitė, Ieva Žutautė, A. Brukštus

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引用次数: 0

摘要

本研究开发了 4-烷基-6-(5-芳基-1,2,3-噻二唑-4-基)苯-1,3-二醇的高效合成方法，作为潜在的同工酶特异性 Hsp90 抑制剂。合成途径始于市售的 1,3-苯二酚，并采用了众所周知的反应。通过弗里德尔-卡夫斯酰化和羰基还原为亚甲基，得到 1-（5-烷基-2,4-二羟基苯基）-2-芳基乙烷-1-酮。随后与肼基甲酸乙酯进行缩合和 Hurd-Mori 环化反应得到了标题化合物。

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Synthesis of novel 4-alkyl-6-(5-aryl-1,2,3-thiadiazol-4-yl) benzene-1,3-diols as potential Hsp90 inhibitors

The efficient synthesis of 4-alkyl-6-(5-aryl-1,2,3-thiadiazol-4-yl)benzene-1,3-diols as potential isoform-specific Hsp90 inhibitors was developed. The synthetic pathway starts from the commercially available 1,3-benzenediol and employs well-known reactions. The Friedel–Crafts acylation and carbonyl group reduction to the methylene group gave 1-(5-alkyl-2,4-dihydroxyphenyl)-2-arylethan-1-ones. The subsequently carried out condensation with ethyl carbazate and Hurd–Mori cyclisation gave title compounds.

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来源期刊

Chemija 化学-化学综合

CiteScore

1.30

自引率

16.70%

发文量

审稿时长

>12 weeks

期刊介绍： Chemija publishes original research articles and reviews from all branches of modern chemistry, including physical, inorganic, analytical, organic, polymer chemistry, electrochemistry, and multidisciplinary approaches.