4-Bromo-1-isoquinolinamine → 2-(1-((2-(1-Aminoisoquinolin-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperidin-4-yl)propan-2-ol
Reaktionsgleichung
Cl[C:2]1[N:3]=[C:4]([N:22]2[CH2:27][CH2:26][O:25][CH2:24][CH2:23]2)[C:5]2[S:10][C:9]([CH2:11][N:12]3[CH2:17][CH2:16][CH:15]([C:18]([OH:21])([CH3:20])[CH3:19])[CH2:14][CH2:13]3)=[CH:8][C:6]=2[N:7]=1.Br[C:29]1[C:38]2[C:33](=[CH:34][CH:35]=[CH:36][CH:37]=2)[C:32]([NH2:39])=[N:31][CH:30]=1>>[NH2:39][C:32]1[C:33]2[C:38](=[CH:37][CH:36]=[CH:35][CH:34]=2)[C:29]([C:2]2[N:3]=[C:4]([N:22]3[CH2:27][CH2:26][O:25][CH2:24][CH2:23]3)[C:5]3[S:10][C:9]([CH2:11][N:12]4[CH2:17][CH2:16][CH:15]([C:18]([OH:21])([CH3:20])[CH3:19])[CH2:14][CH2:13]4)=[CH:8][C:6]=3[N:7]=2)=[CH:30][N:31]=1Komponenten
3
Versuchsvorschrift
Following the procedures for 108, 2-(1-((2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperidin-4-yl)propan-2-ol and 4-bromoisoquinolin-1-amine were converted to 130. LCMS: M+H+=519. 1H NMR (400 MHz, DMSO) δ 8.99 (d, J=8.5, 1H), 8.58 (s, 1H), 8.26 (d, J=8.5, 1H), 8.17 (s, 2H), 7.68 (t, J=7.6, 1H), 7.50 (t, J=7.5, 1H), 7.37 (s, 1H), 7.12 (s, 1H), 4.00-3.89 (m, 4H), 3.86-3.75 (m, 6H), 2.99 (d, J=11.0, 2H), 1.97 (t, J=11.2, 2H), 1.65 (t, J=15.4, 2H), 1.37-1.11 (m, 3H), 1.04 (s, 6H)