3-(4-Methylpiperazin-1-yl)aniline → [8-(4-Methanesulfonyl-phenoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[3-(4-methyl-piperazin-1-yl)-phenyl]-amine
反応式
Cl[C:2]1[N:21]=[C:5]2[C:6]([O:10][C:11]3[CH:16]=[CH:15][C:14]([S:17]([CH3:20])(=[O:19])=[O:18])=[CH:13][CH:12]=3)=[CH:7][CH:8]=[CH:9][N:4]2[N:3]=1.[CH3:22][N:23]1[CH2:28][CH2:27][N:26]([C:29]2[CH:30]=[C:31]([CH:33]=[CH:34][CH:35]=2)[NH2:32])[CH2:25][CH2:24]1>>[CH3:20][S:17]([C:14]1[CH:15]=[CH:16][C:11]([O:10][C:6]2[C:5]3[N:4]([N:3]=[C:2]([NH:32][C:31]4[CH:33]=[CH:34][CH:35]=[C:29]([N:26]5[CH2:25][CH2:24][N:23]([CH3:22])[CH2:28][CH2:27]5)[CH:30]=4)[N:21]=3)[CH:9]=[CH:8][CH:7]=2)=[CH:12][CH:13]=1)(=[O:19])=[O:18]参加物
3
実験手順
[8-(4-Methanesulfonyl-phenoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[3-(4-methyl-piperazin-1-yl)-phenyl]-amine was prepared from 2-chloro-8-(4-methanesulfonyl-phenoxy)-[1,2,4]triazolo[1,5-a]pyridine (0.070 g, 0.21 mmol) and 3-(4-methylpiperazin-1-yl)aniline (0.056 g, 0.29 mmol) in a manner analogous to Example 2d. Product was isolated as a tan solid (56 mg, 54%). MP=Softened at 114-119° C. then melted at 199-201° C. 1H NMR (400 MHz, (D3C)2SO, δ, ppm): 9.55 (s, 1H), 8.76 (d, J=6.56 Hz, 1H), 7.89 (d, J=8.00 Hz, 2H), 7.50 (d, J=7.69 Hz, 1H), 7.26 (s, 1H), 7.21 (d, J=8.04 Hz, 2H), 7.10-7.11 (m, 3H), 6.46 (d, J=6.60 Hz, 1H), 3.20 (s, 3H), 3.04 (s, 4H), 2.42 (s, 4H), 2.22 (s, 3H). MS=479 (MH)+.
出典と根拠
- ORDレコード
- ord-84e55564281841e09a64edf852dcbcf9
- 出典データセット
- uspto-grants-2013_08
- 特許番号
- US08501936B2
反応ノート
読み込み中…