反应详情

To a solution of 1-(4-fluorophenyl)-5-[3-((R)-2,2,2-trifluoro-1-methylethoxymethyl)phenyl]-1H-pyrazol-3-ylamine (52 mg) in N,N-dimethylacetamide (0.5 ml) were sequentially added (S)-5-oxopyrrolidine-3-carboxylic acid (20 mg) prepared according to the same procedures as Preparation 5 and WSC.HCl (40 mg) at room temperature, and the mixture was stirred for 0.5 hours. To this reaction mixture was added water, and then the precipitated solid was collected by filtration. This solid was purified by silica gel thin-layer chromatography (eluent: chloroform/methanol=9/1). To the resulting solid were added water and a small amount of methanol, and the mixture was stirred. A solid was collected by filtration from this suspension, and dried under reduced pressure to give the titled compound (37 mg).

1. customprepared
2. filtrationthe precipitated solid was collected by filtration
3. customThis solid was purified by silica gel thin-layer chromatography (eluent: chloroform/methanol=9/1)
4. additionTo the resulting solid were added water
5. stirringa small amount of methanol, and the mixture was stirred
6. filtrationA solid was collected by filtration from this suspension
7. customdried under reduced pressure