反应详情

To a solution of the N-(8-benzyl-8-azabicyclo[3.2.1]oct-3-yl)-4-methyl-1H-indazol-5-amine (130 mg, 0.375 mmol) obtained in Example 500 in ethanol (10 ml) were added 10% Pd-C (26 mg) and then ammonium formate (118 mg, 1.87 mmol), and the resulting mixture was heated under reflux for 1 hour. The solid was removed by filtration using Celite, and the solvent was distilled off under reduced pressure. Ethyl acetate/aqueous ammonia was added to the residue, followed by extraction with ethyl acetate, and the extract solution was washed with a saturated aqueous sodium chloride solution, dried over sodium sulfate, and then distilled under reduced pressure to remove the solvent, whereby N-(8-azabicyclo[3.2.1]oct-3-yl)-4-methyl-1H-indazol-5-amine (84 mg, 88%) was obtained.

1. temperatureunder reflux for 1 hour
2. customThe solid was removed by filtration
3. distillationthe solvent was distilled off under reduced pressure
4. additionEthyl acetate/aqueous ammonia was added to the residue
5. extractionfollowed by extraction with ethyl acetate
6. washthe extract solution was washed with a saturated aqueous sodium chloride solution
7. dry with materialdried over sodium sulfate
8. distillationdistilled under reduced pressure
9. customto remove the solvent