反应详情

To a solution of 1-(4-fluorophenyl)-5-iodo-1H-pyrazol-3-ylamine (84 mg) prepared according to the same procedures as Preparation 18 in 1,4-dioxane (1.0 ml) were sequentially added 2-[3-fluoro-5-((R)-2,2,2-trifluoro-1-methylethoxymethyl)phenyl]-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane (106 mg) prepared according to the same procedures as Preparation 15, palladium (II) acetate (7 mg), tricyclohexylphosphine (17 mg) and a 2M aqueous solution of potassium carbonate (0.5 ml) at room temperature, and the mixture was stirred at 105° C. for 2 hours. This reaction mixture was cooled to room temperature and after removing an aqueous layer, an organic layer was filtered through silica gel (5 g), and subjected to elution with ethyl acetate. The filtrate was concentrated under reduced pressure, and the resulting residue was purified by silica gel thin-layer chromatography (eluent: n-hexane/ethyl acetate=3/2) to give the titled compound.

1. customprepared
2. customafter removing an aqueous layer
3. filtrationan organic layer was filtered through silica gel (5 g)
4. washsubjected to elution with ethyl acetate
5. concentrationThe filtrate was concentrated under reduced pressure
6. customthe resulting residue was purified by silica gel thin-layer chromatography (eluent: n-hexane/ethyl acetate=3/2)