2-Fluoroethyl methanesulfonate → 1-Cyclopropyl-3-(3-fluoro-4-(2-(5-((4-((2-fluoroethyl)(methyl)amino)piperidin-1-yl)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)urea
反応式
CS(O[CH2:6][CH2:7][F:8])(=O)=O.[CH:9]1([NH:12][C:13]([NH:15][C:16]2[CH:21]=[CH:20][C:19]([O:22][C:23]3[CH:28]=[CH:27][N:26]=[C:25]4[CH:29]=[C:30]([C:32]5[CH:37]=[CH:36][C:35]([CH2:38][N:39]6[CH2:44][CH2:43]N(CCF)C[CH2:40]6)=[CH:34][N:33]=5)[S:31][C:24]=34)=[C:18]([F:48])[CH:17]=2)=[O:14])[CH2:11][CH2:10]1>>[CH:9]1([NH:12][C:13]([NH:15][C:16]2[CH:21]=[CH:20][C:19]([O:22][C:23]3[CH:28]=[CH:27][N:26]=[C:25]4[CH:29]=[C:30]([C:32]5[CH:37]=[CH:36][C:35]([CH2:38][N:39]6[CH2:44][CH2:43][CH:9]([N:12]([CH2:6][CH2:7][F:8])[CH3:13])[CH2:10][CH2:40]6)=[CH:34][N:33]=5)[S:31][C:24]=34)=[C:18]([F:48])[CH:17]=2)=[O:14])[CH2:11][CH2:10]1参加物
3
反応物 2
生成物 1
実験手順
Compound 421 (example 269) was prepared in one step by reacting the amine precursor 401 (table 31) with compound 419, similarly to compound 420 (example 268, scheme 77). 1H NMR (400 MHz, DMSO-d6) δ (ppm): 8.73 (s, 1H), 8.54 (d, J=1.6 Hz, 1H), 8.52 (d, J=5.6 Hz, 1H), 8.33 (s, 1H), 8.24 (d, J=8.0 Hz, 1H), 7.85 (dd, J=8.0, 2.0 Hz, 1H), 7.73 (dd, J=13.6, 2.4 Hz, 1H), 7.38 (t, J=9.0 Hz, 1H), 7.22-7.18 (m, 1H), 6.64 (d, J=5.2 Hz, 1H), 6.56 (bd, J=2.8 Hz, 1H), 4.51 (t, J=5.2 Hz, 1H), 4.39 (t, J=5.2 Hz, 1H), 3.54 (s, 2H), 2.90-2.82 (m, 2H), 2.77-2.63 (m, 2H), 2.59-2.50 (m, 1H), 2.40-2.30 (m, 1H), 2.22 (s, 3H), 2.02-1.91 (m, 2H), 1.69-1.61 (m, 2H), 1.50-1.38 (m, 2H), 0.68-0.62 (m, 2H), 0.45-0.40 (m, 2H). MS (m/z): 593.59 (M+H).
出典と根拠
- ORDレコード
- ord-57262cd041694e76bc1c694bf19d08f9
- 出典データセット
- uspto-grants-2014_12
- 特許番号
- US08906852B2
反応ノート
読み込み中…