Water → 5-(1-Dimethylsulfamoyl-1H-imidazol-2-yl)-7-fluoro-3-[(E)-2-(4-fluorophenyl)-vinyl]-indazole-1-sulfonic Acid Dimethylamide

Participants

Reaction Steps

36.5 mg of 7-fluoro-3-[(E)-2-(4-fluorophenyl)-vinyl]-5-(1H-imidazol-2-yl)-1H-indazole obtained by Example 603 was dissolved in N,N-dimethylformamide, and added with 14 mg of sodium hydride (containing 60%) under ice cooling and stirred for 10 minutes. Adding dropwise with 30.3 μl of N,N-dimethylsulfamoyl chloride, the solution was warmed to room temperature and stirred overnight. After stopping the reaction by adding water, the solution was extracted with ethyl acetate, and the organic layer was washed with water and saturated brine. After drying the organic layer over magnesium sulfate, the solvent was evaporated. The crude product was purified by preparative TLC, to afford 14.2 mg of the title compound.

Provenance & Evidence