反応式
[NH2:1][C:2]1[N:7]=[C:6]([N:8]2[C:16]3[C:11](=[CH:12][CH:13]=[C:14](I)[CH:15]=3)[C:10]([C:18]([N:20]([CH3:27])[C:21]3[CH:26]=[CH:25][CH:24]=[CH:23][N:22]=3)=[O:19])=[N:9]2)[CH:5]=[CH:4][N:3]=1.O1C=CN=C1C(O)(C#C)C.[N:38]1[CH:43]=[CH:42][CH:41]=[N:40][C:39]=1[C:44]([OH:48])([C:46]#[CH:47])[CH3:45]>>[NH2:1][C:2]1[N:7]=[C:6]([N:8]2[C:16]3[C:11](=[CH:12][CH:13]=[C:14]([C:47]#[C:46][C:44]([OH:48])([C:39]4[N:40]=[CH:41][CH:42]=[CH:43][N:38]=4)[CH3:45])[CH:15]=3)[C:10]([C:18]([N:20]([CH3:27])[C:21]3[CH:26]=[CH:25][CH:24]=[CH:23][N:22]=3)=[O:19])=[N:9]2)[CH:5]=[CH:4][N:3]=1参加物
4
反応物 3
生成物 1
実験手順
The title compound was prepared according to the procedure described in Example 70-b, by substituting 4-{6-iodo-3-[(morpholin-4-yl)carbonyl]-1H-indazol-1-yl}pyrimidin-2-amine with 1-(2-aminopyrimidin-4-yl)-6-iodo-N-methyl-N-(pyridin-2-yl)indazole-3-carboxamide and 2-(1,3-oxazol-2-yl)but-3-yn-2-ol with 2-(pyrimidin-2-yl)but-3-yn-2-ol in Step 2: 1H NMR (500 MHz, DMSO) delta 1.91 (3H, s), 3.54 (3H, s), 6.25 (1H, s), 6.28 (1H, d, J=5.5 Hz), 7.10 (2H, s), 7.25 (1H, dd, J=6.9, 5.1 Hz), 7.37 (1H, dd, J=8.4, 1.0 Hz), 7.41 (1H, d, J=8.1 Hz), 7.50 (1H, t, J=4.9 Hz), 7.80 (1H, td, J=7.8, 1.8 Hz), 8.00 (1H, d, J=8.4 Hz), 8.19 (1H, d, J=5.4 Hz), 8.32 (1H, d, J=3.4 Hz), 8.80 (1H, s), 8.86-8.96 (2H, m); LC-MS: m/z=+492.15 (M+H)+.
出典と根拠
- ORDレコード
- ord-65fa0d780c3f49639951f8aab3e734a0
- 出典データセット
- uspto-grants-2014_12
- 特許番号
- US08901313B2
関連ノート
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