反应详情

Triethylamine (73 μl) and dimethylsulfamoyl chloride (56 μl) were added to a mixture of 5-methyl-N-[5-methyl-6-(piperidin-4-yl)pyridin-3-yl]-1-[5-(trifluoromethyl)pyridin-2-yl]-1H-pyrazole-4-carboxamide (222 mg) described in Reference Example 171 and dichloromethane (10 ml), stirred at room temperature for 6.5 hours, triethylamine (146 μl) and dimethylsulfamoyl chloride (56 μl) were added and stirred at room temperature for 7.5 hours. Water was added to the reaction solution, extracted with chloroform, the organic layer was washed with saturated brine, dried over anhydrous sodium sulfate and concentrated in vacuo. The precipitated solid was washed with ethyl acetate and ethanol to give the titled compound (122 mg) as a white solid.

1. stirringstirred at room temperature for 7.5 hours
2. extractionextracted with chloroform
3. washthe organic layer was washed with saturated brine
4. dry with materialdried over anhydrous sodium sulfate
5. concentrationconcentrated in vacuo
6. washThe precipitated solid was washed with ethyl acetate and ethanol