反应详情

Triethylamine (2.6 mL, 18.7 mmol) was added to a solution of 5-bromo-3-(4-piperidinyl)-1H-indole-7-carboxamide hydrochloride in DMF (15 mL) at 0° C. The mixture was stirred at room temperature for 10 min, and 2-propanesulfonyl chloride (1.04 mL, 9.32 mmol) was added. Stirring continued for another 30 min, and the reaction mixture was diluted with 1:1 EtOAc/H2O (200 mL). The layers were separated, and the aqueous layer was extracted with EtOAc (2×50 mL). The combined organic layers were washed with saturated NaCl (1×100 mL), dried (MgSO4), and concentrated under reduced pressure. The crude product was washed with MeOH (2×10 mL) to give the title compound (1.5 g, 75%).

1. stirringStirring
2. waitcontinued for another 30 min
3. customThe layers were separated
4. extractionthe aqueous layer was extracted with EtOAc (2×50 mL)
5. washThe combined organic layers were washed with saturated NaCl (1×100 mL)
6. dry with materialdried (MgSO4)
7. concentrationconcentrated under reduced pressure
8. washThe crude product was washed with MeOH (2×10 mL)