Acryloyl chloride → 1-(4-(((5-Fluoro-3-(4-phenoxyphenyl)pyridin-2-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one
反応式
Br[C:2]1[C:3](Cl)=[N:4][CH:5]=[C:6]([F:8])[CH:7]=1.[NH2:10][CH2:11][CH:12]1[CH2:17][CH2:16][N:15]([C:18]([O:20]C(C)(C)C)=O)[CH2:14][CH2:13]1.[O:25]([C:32]1[CH:37]=[CH:36][C:35](B(O)O)=[CH:34][CH:33]=1)[C:26]1[CH:31]=[CH:30][CH:29]=[CH:28][CH:27]=1.[C:41](Cl)(=O)[CH:42]=C>>[F:8][C:6]1[CH:7]=[C:2]([C:29]2[CH:30]=[CH:31][C:26]([O:25][C:32]3[CH:37]=[CH:36][CH:35]=[CH:34][CH:33]=3)=[CH:27][CH:28]=2)[C:3]([NH:10][CH2:11][CH:12]2[CH2:13][CH2:14][N:15]([C:18](=[O:20])[CH:41]=[CH2:42])[CH2:16][CH2:17]2)=[N:4][CH:5]=1参加物
5
実験手順
1-(4-(((5-fluoro-3-(4-phenoxyphenyl)pyridin-2-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one was prepared from 3-bromo-2-chloro-5-fluoropyridine, tert-butyl 4-(aminomethyl)piperidine-1-carboxylate, (4-phenoxyphenyl)boronic acid, and acryloyl chloride using methods B, C, D, and F. HPLC purity: 99%. MS: m/z=432 [M+H]+. 1H-NMR (DMSO-d6) δ 8.01 (s, 1H), 7.47-7.45 (m, 4H), 7.32 (d, 1H), 7.21 (t, 1H), 7.12-7.09 (m, 4H), 6.82-6.75 (m, 1H), 6.07 (d, 1H), 5.82 (broad s, 1H), 5.64 (d, 1H), 4.39 (d, 1H), 4.02 (d, 1H), 3.18 (d, 2H), 2.99 (t, 1H), 2.59 (t, 1H), 1.92 (s, 1H), 1.68 (m, 2H), 1.00 (m, 2H).
出典と根拠
- ORDレコード
- ord-bdd914e6dcd44df6a1af38cfa32e2b27
- 出典データセット
- uspto-grants-2015_07
- 特許番号
- US09073947B2
反応ノート
読み込み中…