1-[2-(4-Aminopiperidin-1-yl)ethyl]-2-oxo-1,2-dihydroquinoline-7-carbonitrile → 1-[2-(4-Aminopiperidin-1-yl)ethyl]-7-bromo-1H-pyrido[2,3-b][1,4]oxazin-2(3H)-one
反応式
[Br:1][C:2]1[CH:28]=[N:27][C:5]2[O:6][CH2:7][C:8](=[O:26])[N:9]([CH2:10][CH2:11][N:12]3[CH2:17][CH2:16][CH:15]([NH:18]C(=O)OC(C)(C)C)[CH2:14][CH2:13]3)[C:4]=2[CH:3]=1.NC1CCN(CCN2C3C(=CC=C(C#N)C=3)C=CC2=O)CC1>>[NH2:18][CH:15]1[CH2:14][CH2:13][N:12]([CH2:11][CH2:10][N:9]2[C:8](=[O:26])[CH2:7][O:6][C:5]3[N:27]=[CH:28][C:2]([Br:1])=[CH:3][C:4]2=3)[CH2:17][CH2:16]1参加物
3
反応物 2
生成物 1
実験手順
tert-Butyl {1-[2-(7-bromo-2-oxo-2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-1-yl)ethyl]piperidin-4-yl}carbamate (Intermediate 210) (0.85 g) was reacted as described for Intermediate 14. The crude trifluoro acetate of the title compound was used without further purification for the next step (quantitative yield).