Ethyl 5-benzylamino-6,7-difluoro-1,4-dihydro-4-oxo-1-(tetrahydropyran-4-yl)-3-quinolinecarboxylate → Ethyl 5-amino-6,7-difluoro-1,4-dihydro-4-oxo-1-(tetrahydropyran-4-yl)-3-quinolinecarboxylate
反応式
C([NH:8][C:9]1[C:18]([F:19])=[C:17]([F:20])[CH:16]=[C:15]2[C:10]=1[C:11](=[O:32])[C:12]([C:27]([O:29][CH2:30][CH3:31])=[O:28])=[CH:13][N:14]2[CH:21]1[CH2:26][CH2:25][O:24][CH2:23][CH2:22]1)C1C=CC=CC=1>CC(O)=O.[Pd]>[NH2:8][C:9]1[C:18]([F:19])=[C:17]([F:20])[CH:16]=[C:15]2[C:10]=1[C:11](=[O:32])[C:12]([C:27]([O:29][CH2:30][CH3:31])=[O:28])=[CH:13][N:14]2[CH:21]1[CH2:22][CH2:23][O:24][CH2:25][CH2:26]1参加物
4
実験手順
To a suspension of ethyl 5-benzylamino-6,7-difluoro-1,4-dihydro-4-oxo-1-(tetrahydropyran-4-yl)-3-quinolinecarboxylate (112 mg, 0.252 mmol) in AcOH (5 mL), was added 10% Pd—C (11.2 mg), the whole mixture was stirred at room temperature for 4 h under H2 atmosphere (1 atm). After insoluble materials were filtered off, the filtrate was concentrated in vacuo. Flash chromatography of the residue (EtOAc) gave ethyl 5-amino-6,7-difluoro-1,4-dihydro-4-oxo-1-(tetrahydropyran-4-yl)-3-quinolinecarboxylate (76.5 mg, 86%) as pale yellow powder.