Isoquinolin-3-Amine → 3-[7-Fluoro-2-(4-fluoro-benzyl)-3-oxo-2,3-dihydro-1H-isoindol-1-yl]-N-isoquinolin-3-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].C1C2[C:38](=CC=CC=2)[CH:37]=[C:36](N)N=1>>[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[N:17]=[CH:18][C:19]3[C:23]([CH:24]=1)=[CH:38][CH:37]=[CH:36][CH:20]=3)=[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 isoquinolin-3-amine (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 (95 mg, 35%). 1HNMR (300 MHz, CDCl3) δ 8.28 (d, J=9 Hz, 1H), 8.15 (d, J=9 Hz, 1H), 7.91 (s, 1H), 7.75 (m, 2H), 7.70 (d, J=8 Hz, 1H), 7.64 (m, 1H), 7.45 (m, 2H), 7.32 (m, 2H), 7.20 (t, J=9 Hz, 1H), 7.02 (m, 2H), 5.29 (d, J=15 Hz, 1H), 4.71 (m, 1H), 4.26 (d, J=15 Hz, 1H), 2.55 (m, 2H), 2.00 (m, 2H). MS: m/z (MH+) 458.