反应详情

43 mg of triphosgene followed by 110 μl of triethylamine at 0° C. are added to a solution of 100 mg of 3-(4-aminophenyl)-1H-indole-2-carboxamide (example 1) in 18 ml of tetrahydrofuran. The mixture is stirred for one hour at ambient temperature and then 110 mg of 5-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylamine are added. The mixture is stirred for one hour and concentrated under reduced pressure, and the residue is triturated with 2 ml of ethyl acetate, to give a white solid. After filtration and drying, 150 mg of 3-{4-[3-(5-tertbutyl-2-p-tolyl-2H-pyrazol-3-yl)ureido]phenyl}-1H-indole-2-carboxamide are obtained, the characteristics of which are as follows:

1. stirringThe mixture is stirred for one hour
2. concentrationconcentrated under reduced pressure
3. customthe residue is triturated with 2 ml of ethyl acetate
4. customto give a white solid
5. filtrationAfter filtration
6. customdrying