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Issue 22, 2006
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Microwave-assisted synthesis of N-pyrazole ureas and the p38α inhibitor BIRB 796 for study into accelerated cell ageing

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Abstract

Microwave irradiation of substituted hydrazines and β-ketoesters gives 5-aminopyrazoles in excellent yield, which can be transformed to the corresponding N-carbonyl derivatives by treatment with an isocyanate or chloroformate. Derivatization of 4-nitronaphth-1-ol using predominantly microwave heating methods and reaction with an N-pyrazole carbamate provides a rapid route to the N-pyrazole urea BIRB 796 in high purity, as a potent and selective inhibitor of p38α mitogen-activated protein kinase for the study of accelerated ageing in Werner syndrome cells.

Graphical abstract: Microwave-assisted synthesis of N-pyrazole ureas and the p38α inhibitor BIRB 796 for study into accelerated cell ageing

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Publication details

The article was received on 09 Aug 2006, accepted on 22 Sep 2006 and first published on 09 Oct 2006


Article type: Paper
DOI: 10.1039/B611493H
Citation: Org. Biomol. Chem., 2006,4, 4158-4164

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    Microwave-assisted synthesis of N-pyrazole ureas and the p38α inhibitor BIRB 796 for study into accelerated cell ageing

    M. C. Bagley, T. Davis, M. C. Dix, C. S. Widdowson and D. Kipling, Org. Biomol. Chem., 2006, 4, 4158
    DOI: 10.1039/B611493H

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