反应详情

2-[1-(4-{[5-Nitro-2-(2-trifluoromethoxy-benzylamino)-pyrimidin-4-ylamino]-methyl}-cyclohexyl)-azetidin-3-yl]-isoindole-1,3-dione (92 mg, 0.15 mmol) was dissolved in EtOH-CH2Cl2 (3 mL, 2:1). With stirring, hydrazine monohydrate (11.3 mg, 0.23 mmol) was added and the reaction was stirred at 25° C. for 3 h. The volatiles were removed in vacuo and the crude residue was purified via flash chromatography (SiO2, 1:9:90-NH4OH:CH3OH:CH2Cl2) to afford 46 mg (62%) of the target compound, m/z 496.35 [M+1]+.

1. stirringthe reaction was stirred at 25° C. for 3 h
2. customThe volatiles were removed in vacuo
3. customthe crude residue was purified via flash chromatography (SiO2, 1:9:90-NH4OH:CH3OH:CH2Cl2)