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

被引:79
作者
Bagley, Mark C.
Davis, Terence
Dix, Matthew C.
Widdowson, Caroline S.
Kipling, David
机构
[1] Cardiff Univ, Sch Chem, Cardiff CF10 3AT, S Glam, Wales
[2] Cardiff Univ, Sch Med, Dept Pathol, Cardiff CF14 4XN, S Glam, Wales
基金
英国生物技术与生命科学研究理事会;
关键词
D O I
10.1039/b611493h
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Microwave irradiation of substituted hydrazines and beta-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 p38 alpha mitogen-activated protein kinase for the study of accelerated ageing in Werner syndrome cells.
引用
收藏
页码:4158 / 4164
页数:7
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