反应详情

Stir under N2 a suspension of 3-(4-pyridinylamino)-1H-indole-2-carboxylic acid (0.2 g, 0.78 mmol) in dimethylformamide, add pyridine (0.13 mL, 1.6 mmol) and then add dropwise pentafluorophenyl trifluoroacetate (0.31 g, 1.13 mmol). Stir the reaction overnight at ambient temperature and quench into water. Extract the aqueous mixture with ethyl acetate, wash with 5% aqueous potassium carbonate, brine and dry over MgSO4. Concentrate under vacuum to afford a crude solid, which is triturated with ether to obtain 0.13 g (41%) of the title compound: MS 420(M+H).

1. stirringStir
2. customthe reaction overnight at ambient temperature
3. customquench into water
4. extractionExtract the aqueous mixture with ethyl acetate
5. washwash with 5% aqueous potassium carbonate, brine
6. dry with materialdry over MgSO4
7. concentrationConcentrate under vacuum
8. customto afford a crude solid, which
9. customis triturated with ether