反应详情

A mixture of 1-(4-amino-3-(methylamino)phenyl)-4-((4-fluorobenzyl)oxy)pyridin-2(1H)-one (67.9 mg), 4-ethyl-1,3-oxazole-5-carboxylic acid (28.2 mg), HATU (80.0 mg), N,N-diisopropylethylamine (0.105 ml) and DMF (2.0 ml) was stirred at room temperature for 2 h. The mixture was poured into saturated NaHCO3 solution and extracted with EtOAc. The extract was washed with brine, dried over MgSO4, concentrated in vacuo. The residue was dissolved in AcOH (1.5 ml), and the mixture was stirred at 80° C. for 1 h. The mixture was concentrated in vacuo. The residue was purified by NH silica gel column chromatography (hexane/EtOAc then EtOAc/MeOH). The resulting solid was recrystallized from EtOAc-hexane to give the title compound (15.7 mg) as a white solid.

1. extractionextracted with EtOAc
2. washThe extract was washed with brine
3. dry with materialdried over MgSO4
4. concentrationconcentrated in vacuo
5. dissolutionThe residue was dissolved in AcOH (1.5 ml)
6. stirringthe mixture was stirred at 80° C. for 1 h
7. concentrationThe mixture was concentrated in vacuo
8. customThe residue was purified by NH silica gel column chromatography (hexane/EtOAc
9. customThe resulting solid was recrystallized from EtOAc-hexane