反应详情

To a suspension of 1H-indazol-5-ol (134 mg, 0.999 mmol) in tetrahydrofuran (4 ml) were added tert-butyl 4-hydroxy-1-piperidinecarboxylate (201 mg, 0.999 mmol) and triphenylphosphine (262 mg, 0.999 mmol) at room temperature, followed by adding thereto diethyl azodicarboxylate (0.46 ml, 1.01 mmol) at 0° C., and the resulting mixture was stirred at 0° C. for 30 minutes and then at room temperature for 4 hours. Subsequently, the solvent of the reaction mixture was distilled off under reduced pressure and the resulting residue was purified by a silica gel column chromatography (eluent: hexane/ethyl acetate=7/3) to obtain tert-butyl 4-(1H-indazol-5-yloxy)-1-piperidinecarboxylate (77 mg, 24%).

1. additionby adding
2. distillationSubsequently, the solvent of the reaction mixture was distilled off under reduced pressure
3. customthe resulting residue was purified by a silica gel column chromatography (eluent: hexane/ethyl acetate=7/3)