反应详情

To a solution of 5-[3-fluoro-5-((R)-2,2,2-trifluoro-1-methylethoxymethyl)phenyl]-1-phenyl-1H-pyrazol-3-ylamine (37 mg) in N,N-dimethylacetamide (1.0 ml) were sequentially added (S)-5-oxopyrrolidine-3-carboxylic acid (16 mg) prepared in Preparation 14 and WSC.HCl (23 mg) at room temperature, the mixture was stirred for 5.2 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 from this suspension by filtration, and was dried under reduced pressure to give the titled compound (20 mg).

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