Short Synthesis of 1-(3-<i>tert</i>-Butyl-1-phenyl-1<i>H</i>-pyrazol-5-yl)-3-(5-(2-morpholinoethoxy)-2<i>H</i>-chromen-8-yl) Urea Derivatives
作者:Xingzhou Li、Xinming Zhou、Zhibing Zheng、Wu Zhong、Junhai Xiao、Song Li
DOI:10.1080/00397910902883603
日期:2009.10.21
efficient synthesis of 1-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(5-(2-morpholinoethoxy)-2H-chromen-8-yl) urea derivatives (1a–c), a novel type of p38 MAPK inhibitors, is described. The Claisen thermalrearrangement of arylpropargyl ethers was employd as a key step to synthesize the chromene core. The solvent effect on the ratio of the resultant two isomers of Claisen thermalrearrangement, namely 2-methylbenzofuran