Tetrahydrofuran → 6-(2-Amino-4-pyrimidinyl)-4-(methyloxy)-1H-indazol-3-amine
反応式
[NH2:1][C:2]1[N:7]=[C:6]([C:8]2[CH:15]=[C:14](OC)[C:11]([C:12]#[N:13])=[C:10](F)[CH:9]=2)[CH:5]=[CH:4][N:3]=1.[OH2:19].[NH2:20][NH2:21].[CH2:22]1COCC1>>[NH2:1][C:2]1[N:7]=[C:6]([C:8]2[CH:15]=[C:14]3[C:11]([C:12]([NH2:13])=[N:20][NH:21]3)=[C:10]([O:19][CH3:22])[CH:9]=2)[CH:5]=[CH:4][N:3]=1参加物
4
反応条件
- 温度
- 90 °C
実験手順
To a slurry of 4-(2-amino-4-pyrimidinyl)-2-fluoro-6-(methyloxy)benzonitrile (0.20 g, 0.82 mmol) in THF (2 mL) was added hydrazine monohydrate (1.3 mL), and the resulting mixture was stirred at 90° C. until the starting material was consumed as judged by LCMS (˜12 hours). The reaction mixture was concentrated to afford the title compound (102 mg, 49%) as a bright yellow solid. LC-MS (ES) m/z=257 [M+H]+. 1H NMR (400 MHz, DMSO-d6): δ 3.94 (s, 3H), 5.06 (s, 2H), 6.65 (s, 2H), 6.97 (s, 1H), 7.16 (d, J=5.3 Hz, 1H), 7.54 (d, J=1.0 Hz, 1H), 8.30 (d, J=5.3 Hz, 1H), 11.67 (bs, 1H).