1-((6-Fluoropyridin-2-yl)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine → N-(1-methyl-1H-pyrazol-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
反応式
FC1N=C(C[N:9]2[C:13]3=[N:14][C:15]([NH:18][C:19]4[CH:20]=[N:21][N:22]([CH3:24])[CH:23]=4)=[N:16][CH:17]=[C:12]3[CH:11]=[N:10]2)C=CC=1>CN(C=O)C>[CH3:24][N:22]1[CH:23]=[C:19]([NH:18][C:15]2[N:14]=[C:13]3[NH:9][N:10]=[CH:11][C:12]3=[CH:17][N:16]=2)[CH:20]=[N:21]1参加物
3
反応条件
- 温度
- 180 °C
実験手順
1-((6-fluoropyridin-2-yl)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine (Example 170) (45 mg, 0.138 mmol) was dissolved in DMF (0.6 ml) in a microwave tube under Nitrogen. This was sealed and heated at 180° C. for 1 h. The mixture was concentrated and purified by prep HPLC to afford 1-46-(dimethylamino)pyridin-2-yl)methyl)-N-(1-methyl-1H-pyrazol-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine as yellowish solid (20 mg, 42% yield). 1H NMR (d6-Acetone) δ 8.88 (s and br s, 2H), 8.06 (s, 1H), 7.99 (s, 1H), 7.61 (s, 1H), 7.40 (t, 1H), 6.49 (d, 1H), 6.24 (br s, 1H), 5.51 (s, 2H), 3.83 (s, 3H), 3.02 (s, 6H); LC-MS method B, (ES+) 350.1, RT=5.06 min.