4.4 Article

Microwave-mediated synthesis and manipulation of a 2-substituted-5-aminooxazole-4-carbonitrile library

Journal

TETRAHEDRON LETTERS
Volume 53, Issue 13, Pages 1656-1659

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2012.01.081

Keywords

Microwave-assisted synthesis; Oxazoles; Parallel synthesis; Flow chemistry

Funding

  1. X-ray crystallography unit
  2. Avexa

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A 2-substituted-5-aminooxazole-4-carbonitrile library has been synthesised and modified via microwave-mediated and flow chemistries. One synthesised compound, 5-(1H-pyrrol-1-yl)-4-(1H-tetrazol-5-yl)-2-(thien-2-yl)oxazole, contains three distinct heterocycles attached to the central oxazole core, highlighting the structural diversity of this approach. Three oxazoles had micromolar k(i) values against cannabinoid (CB1/CB2) receptors. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.

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