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

Bagley, Mark C., Davis, Terence ORCID: https://orcid.org/0000-0003-2780-0262, Dix, Matthew C., Widdowson, Caroline S. and Kipling, David Glyn 2006. Microwave-assisted synthesis of N-pyrazole ureas and the p38α inhibitor BIRB 796 for study into accelerated cell ageing. Organic & Biomolecular Chemistry 4 (22) , pp. 4158-4164. 10.1039/b611493h

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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.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Chemistry Medicine
Subjects:	R Medicine > R Medicine (General)
Publisher:	Royal Society of Chemistry
ISSN:	1477-0520
Last Modified:	14 Dec 2022 07:21
URI:	https://orca.cardiff.ac.uk/id/eprint/63543

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