反应详情

温度

130 °C

A flask was charged with 1H-indazol-5-ol (0.89 g, 0.66 mmol), (R)-tert-butyl 4-(3-(methylsulfonyloxy)-2-oxopyrrolidin-1-yl)piperidine-1-carboxylate (Preparation D; 0.2 g, 0.55 mmol), K2CO3 (0.092 g, 0.66 mmol), and DMSO (4 mL). The reaction was stirred at 130° C. overnight. Added water and extracted with ethyl acetate. The organic layers were combined, dried, filtered and concentrated. The residue was purified using silica gel column chromatography with 50-100% ethyl acetate in hexanes to provide (S)-tert-butyl 4-(3-(1H-indazol-5-yloxy)-2-oxopyrrolidin-1-yl)piperidine-1-carboxylate (0.198 g, 90% yield).

1. extractionAdded water and extracted with ethyl acetate
2. customdried
3. filtrationfiltered
4. concentrationconcentrated
5. customThe residue was purified