反应详情

6-Nitro-1H-indazole (12.26 mmol, 2 g), tert-butyl 4-(methylsulfonyloxy)piperidine-1-carboxylate (12.26 mmol, 3.42 g) and potassium carbonate (24.52 mmol, 3.39 g) were combined and heated to 100° C. in N,N-dimethylformamide (40 mL) for 4 hours. The reaction mixture was diluted with ethyl acetate and washed with water. The organic phase was dried over sodium sulfate and concentrated at reduced pressure. The resulting residue was purified by silica chromatography (eluting with a solvent gradient from 20% ethyl acetate/heptane to 60% ethyl acetate/heptane) to afford the title compound (1.045 g). MS (ESI) m/z 347.2 [M+H]+

1. washwashed with water
2. dry with materialThe organic phase was dried over sodium sulfate
3. concentrationconcentrated at reduced pressure
4. customThe resulting residue was purified by silica chromatography (
5. washeluting with a solvent gradient from 20% ethyl acetate/heptane to 60% ethyl acetate/heptane)