4.3 Article

Versatile approaches to a library of building blocks based on 5-acylthiazole skeleton

Journal

SYNTHETIC COMMUNICATIONS
Volume 50, Issue 23, Pages 3616-3628

Publisher

TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2020.1808224

Keywords

Building blocks; Hantzsch thiazole synthesis; Leuckart-Wallach reaction; oxime; thiazole

Funding

  1. Ministry of Education and Science of Ukraine [0118U002025]
  2. V.N. Karazin Kharkiv National University [811H/11-09, 811H/38-09, 811 H/19-12]

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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(1)H and(13)C NMR-spectroscopy, elemental analysis, and mass-spectrometry.

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