2-Aminoquinoline → 3-[7-Fluoro-2-(4-fluoro-benzyl)-3-oxo-2,3-dihydro-1H-isoindol-1-yl]-N-quinolin-2-yl-propionamide
反応式
[F:1][C:2]1[CH:3]=[CH:4][CH:5]=[C:6]2[C:10]=1[CH:9]([CH2:11][CH2:12][C:13]([NH:15][C:16]1[CH:24]=[CH:23][C:19]([C:20](O)=O)=[CH:18][N:17]=1)=[O:14])[N:8]([CH2:25][C:26]1[CH:31]=[CH:30][C:29]([F:32])=[CH:28][CH:27]=1)[C:7]2=[O:33].N1C2C(=CC=CC=2)[CH:37]=[CH:36][C:35]=1N>>[F:1][C:2]1[CH:3]=[CH:4][CH:5]=[C:6]2[C:10]=1[CH:9]([CH2:11][CH2:12][C:13]([NH:15][C:16]1[CH:24]=[CH:23][C:19]3[C:18](=[CH:35][CH:36]=[CH:37][CH:20]=3)[N:17]=1)=[O:14])[N:8]([CH2:25][C:26]1[CH:27]=[CH:28][C:29]([F:32])=[CH:30][CH:31]=1)[C:7]2=[O:33]参加物
3
実験手順
The product from Example 11, Part D (200 mg, 0.6 mmol) and quinolin-2-ylamine (131 mg, 0.91 mmol) were converted to the title compound in a manner analogous to the method described in Example 7, Part E, using CH2Cl2 in place of THF in the reaction and EtOAc in the workup, and without crystallization (220 mg, 80%). 1HNMR (400 MHz, CDCl3) δ 8.87 (s, 1H), 8.46 (s, 1H), 8.09 (s, 1H), 7.87 (d, J=8 Hz, 1H), 7.80 (d, J=8 Hz, 1H), 7.66 (m, 2H), 7.48 (t, J=7 Hz, 1H), 7.41 (m, 1H), 7.32 (m, 2H), 7.16 (t, J=9 Hz, 1H), 7.01 (t, J=7 Hz, 2H), 5.30 (d, J=15 Hz, 1H), 4.71 (m, 1H), 4.25 (d, J=15 Hz, 1H), 2.59 (m, 2H), 1.98 (m, 2H). MS: m/z (MH+) 458.
出典と根拠
- ORDレコード
- ord-e15482c1bb254c5fa83e281564f77f88
- 出典データセット
- uspto-grants-2014_08
- 特許番号
- US08796313B2
反応ノート
読み込み中…