反应详情

温度

40 °C

1-[6-(2-t-Butylsulfamoylphenyl)pyridin-3-ylmethyl]-5-propyl-1H-pyrazole-3-carboxylic acid (480 mg, 1.0 mmol) was dissolved in TFA (2.8 mL, 36.8 mmol) and heated at 40° C. for 3 hours. The mixture was diluted with toluene and concentrated (azeotrope ×3). The residue was dissolved in DCM (5.53 mL, 86.2 mmol), then triethylamine (1.8 mL, 12.6 mmol) and acetic anhydride (992 μL, 10.5 mmol) were added. The resulting solution was stirred at room temperature for 1 hour. Additional triethylamine and acetic anhydride were added to drive the reaction. The reaction was then quenched with water (150 μL) and dried through azeotrope with toluene to yield the title compound (108 mg), which was used without further purification.

1. concentrationconcentrated (azeotrope ×3)
2. customthe reaction
3. customThe reaction was then quenched with water (150 μL)
4. dry with materialdried through azeotrope with toluene