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

A library of oxazoles is synthesised using parallel synthetic methodology. 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, con...

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Veröffentlicht in:Tetrahedron letters 2012-03, Vol.53 (13), p.1656-1659
Hauptverfasser: Spencer, John, Patel, Hiren, Amin, Jahangir, Callear, Samantha K., Coles, Simon J., Deadman, John J., Furman, Christophe, Mansouri, Roxane, Chavatte, Philippe, Millet, Régis
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Sprache:eng
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Zusammenfassung:A library of oxazoles is synthesised using parallel synthetic methodology. 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 ki values against cannabinoid (CB1/CB2) receptors.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2012.01.081