Bagley Mark C, Davis Terence, Dix Matthew C, Widdowson Caroline S, Kipling David
School of Chemistry, Main Building, Cardiff University, Park Place, Cardiff, UK.
Org Biomol Chem. 2006 Nov 21;4(22):4158-64. doi: 10.1039/b611493h.
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 p38alpha mitogen-activated protein kinase for the study of accelerated ageing in Werner syndrome cells.
用微波辐射取代肼和β-酮酯可高产率地得到5-氨基吡唑，通过用异氰酸酯或氯甲酸酯处理，可将其转化为相应的N-羰基衍生物。主要使用微波加热方法对4-硝基萘-1-醇进行衍生化，并与N-吡唑氨基甲酸酯反应，可快速获得高纯度的N-吡唑脲BIRB 796，它是一种有效且选择性的p38α丝裂原活化蛋白激酶抑制剂，用于研究沃纳综合征细胞中的加速衰老。
