反应详情

To a suspension of 4-piperidin-1-yl-butyric acid (621.0 mg, 3.0 mmol, 1.5 eq) in 1,2-dichloroethane (6 mL), N,N′-carbonyldiimidazole (453.0 mg, 2.8 mmol, 1.4 eq) was added and the mixture was stirred at room temperature for 1 hour. 5-(1H-indol-3-yl)-2H-pyrazol-3-ylamine (400.0 mg, 2.0 mmol, 1.0 eq) in 1,2-dichloroethane (6 mL) was added; the reaction was stirred at room temperature for 2 days, then 1 day at 70° C., to allow complete migration of the acyl group from the ring nitrogen to the exocyclic nitrogen. The reaction then was allowed to cool down to room temperature and the mixture was washed with saturated Na2CO3 and evaporated under reduced pressure; the crude was purified by preparative HPLC to give 320.0 mg (yield: 41%) of the title compound as formate salt.

1. additionwas added
2. stirringthe reaction was stirred at room temperature for 2 days
3. custom1 day
4. customat 70° C.
5. customThe reaction
6. temperatureto cool down to room temperature
7. washthe mixture was washed with saturated Na2CO3
8. customevaporated under reduced pressure
9. customthe crude was purified by preparative HPLC