反应详情

To trans-2-{2,2-dimethyl-5-[(4-methyl-1H-indazol-5-yl)oxy]cyclohexyl}-1H-isoindole-1,3(2H)-dione was added 30%-methylamine/ethanol (10 ml) at room temperature, and the resulting mixture was refluxed for 8 hours. The reaction solution was concentrated under reduced pressure at room temperature and the resulting residue was purified by a silica gel column chromatography (eluent: chloroform→chloroform/methanol/(1%-aqueous ammonia)=20/1) to obtain trans-2,2-dimethyl-5-[(4-methyl-1H-indazol-5-yl)oxy]cyclohexanamine (143 mg, 60%, containing about 10% of cis isomer).

1. temperaturethe resulting mixture was refluxed for 8 hours
2. concentrationThe reaction solution was concentrated under reduced pressure at room temperature
3. customthe resulting residue was purified by a silica gel column chromatography (eluent: chloroform→chloroform/methanol/(1%-aqueous ammonia)=20/1)