α,α‐Dibromoketone precursors in the synthesis of some new thiazole derivatives: Thiazol‐2‐yl hydrazonobutanoates, thiazol‐2‐yl pyrazole‐4‐carboxylates and acids,Journal of Heterocyclic Chemistry

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α,α‐Dibromoketone precursors in the synthesis of some new thiazole derivatives: Thiazol‐2‐yl hydrazonobutanoates, thiazol‐2‐yl pyrazole‐4‐carboxylates and acids
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-02-21 , DOI: 10.1002/jhet.3937
Vijay Kiran ₁ , Radhika Joshi ₂ , Rashmi Pundeer ₁

Affiliation

In the present study, α,α‐dibromoacetophenones are used as efficient precursors for the facile synthesis of several new hydrazonothiazoles, ethyl 3‐((4‐arylthiazol‐2‐yl)hydrazono)butanoates, which undergo Vilsmeier‐Haack cyclization to obtain thiazolylpyrazole esters, ethyl 3‐methyl‐1‐(4‐arylthiazol‐2‐yl)‐1H‐pyrazole‐4‐carbxylates, basic hydrolysis of which gives the corresponding acids, 3‐methyl‐1‐(4‐arylthiazol‐2‐yl)‐1H‐pyrazole‐4‐carbxylic acids. All these compounds are tested for antibacterial activity against Gram‐positive bacteria Staphylococcus aureus and Bacillus subtilis; Gram‐negative bacteria Escherichia coli and Pseudomonas aeruginosa and antifungal activity against Saccharomyces cerevisiae and Candida albicans.

中文翻译：

某些新型噻唑衍生物合成中的α，α-二溴酮前体：噻唑-2-基肼基丁酸酯，噻唑-2-基吡唑-4-羧酸盐和酸

在本研究中，α，α-二溴苯乙酮被用作有效的前体，用于轻松合成几种新的肼基三唑，3-（（4-芳基噻唑-2-基）肼基）丁酸乙酯，将其经过Vilsmeier-Haack环化反应获得噻唑基吡唑酯，3-甲基-1-（4-芳基噻唑-2-基）-1 H-吡唑-4-羰基酸酯，对其进行碱性水解可得到相应的酸3-甲基-1-（4-芳基噻唑-2-基） yl）-1 H-吡唑-4-碳羟基酸。测试所有这些化合物对革兰氏阳性细菌金黄色葡萄球菌和枯草芽孢杆菌的抗菌活性；革兰氏阴性细菌大肠杆菌和铜绿假单胞菌及其抗真菌活性酿酒酵母和白色念珠菌。

更新日期：2020-02-21

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