反应详情

To a mixture of 0.051 g (0.2 mmole) of toluene-4-sulfonic acid cyclohexyl ester, 0.037 g (0.1 mmole) of 4-(3-chloro-phenyl)-2-(6-hydroxy-benzoimidazol-1-yl)-thiazole-5-carboxylic acid amide (I.25d) and 1 mL of dimethylformamide was added 0.163 g (0.5 mmole) of cesium carbonate. The mixture was heated at 100 degrees for 30 minutes. The mixture was cooled, the solid was removed by filtration and the filtrate purified by reverse phase silica gel chromatography, eluting with acetonitrile-water (gradient 40:60-100:0) to give 0.027 g of 4-(3-chloro-phenyl)-2-(6-cyclohexyloxy-benzoimidazol-1-yl)-thiazole-5-carboxylic acid amide (I.25) as a white powder. MH+/Z=453

1. temperatureThe mixture was heated at 100 degrees for 30 minutes
2. temperatureThe mixture was cooled
3. customthe solid was removed by filtration
4. customthe filtrate purified by reverse phase silica gel chromatography
5. washeluting with acetonitrile-water (gradient 40:60-100:0)