反应详情

Tert-butyl [2-({4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]benzoyl}amino)-4-(2-thienyl)phenyl]carbamate (4.4 g, 7.95 mmol) and hydrazine (0.495 mL, 15.90 mmol) were stirred in refluxing EtOH (35 mL) for 5 hours. Room temperature was attained and the white precipitate removed by filtration and washed with EtOH. The filtrate was concentrated in vacuo and purified by MPLC (1-12.5% [MeOH+1% NH4OH]-DCM) to give tert-butyl [2-{[4-(aminomethyl)benzoyl]amino}-4-(2-thienyl)phenyl]carbamate as a white solid.

1. customRoom temperature
2. customthe white precipitate removed by filtration
3. washwashed with EtOH
4. concentrationThe filtrate was concentrated in vacuo
5. custompurified by MPLC (1-12.5% [MeOH+1% NH4OH]-DCM)