2-Morpholinoethylamine → 9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-N3-(2-morpholinoethyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2,3-dicarboxamide
反応式
[C:1]([C:4]1[N:5]=[C:6]2[C:12]3[CH:13]=[C:14]([C:18]#[C:19][C:20]([OH:23])([CH3:22])[CH3:21])[C:15]([F:17])=[CH:16][C:11]=3[O:10][CH2:9][CH2:8][N:7]2[C:24]=1[C:25]([OH:27])=O)(=[O:3])[NH2:2].[NH2:28][CH2:29][CH2:30][N:31]1[CH2:36][CH2:35][O:34][CH2:33][CH2:32]1>>[F:17][C:15]1[C:14]([C:18]#[C:19][C:20]([OH:23])([CH3:21])[CH3:22])=[CH:13][C:12]2[C:6]3[N:7]([C:24]([C:25]([NH:28][CH2:29][CH2:30][N:31]4[CH2:36][CH2:35][O:34][CH2:33][CH2:32]4)=[O:27])=[C:4]([C:1]([NH2:2])=[O:3])[N:5]=3)[CH2:8][CH2:9][O:10][C:11]=2[CH:16]=1参加物
3
反応物 2
生成物 1
実験手順
2-Carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylic acid (0.05 g) was reacted with 4-(2-aminoethyl)morpholine similar to as described in Example 2 to afford 13.3 mg of 9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-N3-(2-morpholinoethyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2,3-dicarboxamide following reverse phase hplc purification. MS (Q1) 486 (M)+. 1H NMR (400 MHz, DMSO) δ 11.06 (s, 1H), 8.61 (d, J=8.4 Hz, 1H), 8.32 (s, 1H), 7.86 (s, 1H), 7.02 (d, J=10.5 Hz, 1H), 5.47 (s, 1H), 5.08-4.77 (m, 2H), 4.61-4.48 (m, 2H), 3.70-3.51 (m, 3H), 3.51-3.35 (m, 1H), 2.49-2.30 (m, 3H), 1.49 (s, 6H).