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Versatile approaches to a library of building blocks based on 5-acylthiazole skeleton
Synthetic Communications ( IF 2.1 ) Pub Date : 2020-09-03 , DOI: 10.1080/00397911.2020.1808224
Olesia G. Kulyk 1 , Dmytro A. Biloborodov 1 , Maksim A. Cherevatenko 1 , Yevhen Y. Shyriakin 1 , Alexander Yu. Lyapunov 2 , Alexander V. Mazepa 3 , Valerii V. Vashchenko 4 , Valeriy D. Orlov 1 , Maksim A. Kolosov 1
Affiliation  

Abstract Thiazole derivatives represent an important class of azole heterocycles with a broad spectrum of biological activity and, therefore, the synthesis of these compounds is of remarkable concern. We present here practical and reliable protocol for synthesis of some 5-acylthiazoles and demonstrate their utility in the preparation of several new series of thiazole-containing building blocks through transformation of 5-acyl function. Specifically, thiazole-based alcohols, oximes, primary, and secondary amines were successively synthesized in good to excellent yields. The chemical structures of obtained compounds were confirmed by 1H and 13C NMR-spectroscopy, elemental analysis, and mass-spectrometry. Graphical Abstract

中文翻译:

基于 5-酰基噻唑骨架的构建块库的通用方法

摘要 噻唑衍生物是一类重要的唑类杂环,具有广泛的生物活性,因此,这些化合物的合成备受关注。我们在此介绍了一些实用且可靠的合成一些 5-酰基噻唑的方案,并展示了它们在通过 5-酰基功能的转化制备几个新系列的含噻唑结构单元中的效用。具体而言,噻唑基醇、肟、伯胺和仲胺以良好到极好的收率连续合成。所得化合物的化学结构经 1H 和 13C NMR 光谱、元素分析和质谱证实。图形概要
更新日期:2020-09-03
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