反応式
[NH2:1][CH2:2][CH2:3][CH:4]([N:6]1[CH2:11][CH2:10][CH:9]([N:12]([CH2:22][C:23]2[CH:24]=[C:25]([CH:28]=[CH:29][C:30]=2[F:31])[C:26]#[N:27])[C:13]2[CH:14]=[C:15]3[C:19](=[CH:20][CH:21]=2)[NH:18][CH:17]=[CH:16]3)[CH2:8][CH2:7]1)[CH3:5].[CH3:32][C:33]1[C:38]([C:39](O)=[O:40])=[C:37]([CH3:42])[N:36]=[CH:35][N:34]=1>>[C:26]([C:25]1[CH:28]=[CH:29][C:30]([F:31])=[C:23]([CH:24]=1)[CH2:22][N:12]([C:13]1[CH:14]=[C:15]2[C:19](=[CH:20][CH:21]=1)[NH:18][CH:17]=[CH:16]2)[CH:9]1[CH2:10][CH2:11][N:6]([CH:4]([CH3:5])[CH2:3][CH2:2][NH:1][C:39]([C:38]2[C:33]([CH3:32])=[N:34][CH:35]=[N:36][C:37]=2[CH3:42])=[O:40])[CH2:7][CH2:8]1)#[N:27]参加物
実験手順
Using general procedure E, 3-{[[1-(3-amino-1-methyl-propyl)-piperidin-4-yl]-(1H-indol-5-yl)-amino]-methyl}-4-fluoro-benzonitrile (see EXAMPLE 244) (45 mg, 0.11 mmol) and 4,6-dimethyl-pyrimidine-5-carboxylic acid (20 mg, 0.13 mmol) afforded COMPOUND 245 as a white solid (35 mg, 60%). 1H NMR (CDCl3) δ 0.88-1.25 (m, 5H), 1.54-1.64 (m, 1H), 1.76-1.92 (m, 3H), 2.13-2.20 (m, 1H), 2.51 (s, 6H), 2.51-2.57 (m, 1H), 2.69-2.84 (m, 3H), 3.31-3.37 (m, 2H), 3.82-3.85 (m, 1H), 3.98 (s, 2H), 6.39 (s, 1H), 6.72 (d, 1H, J=8.6 Hz), 7.00 (s, 1H), 7.08-7.14 (m, 2H), 7.21 (d, 1H, J=8.6 Hz), 7.43-7.45 (m, 1H), 7.65 (d, 1H, J=6.4 Hz), 8.02 (s, 1H), 8.50 (br s, 1H), 8.83 (s, 1H). 13C NMR (CDCl3) δ 13.74, 22.36, 29.89, 30.88, 31.26, 40.33, 43.81, 44.17, 52.34, 60.54, 60.81, 102.63, 108.63, 110.70, 111.94, 116.61, 116.72, 116.92, 118.91, 125.26, 128.77, 131.10, 132.79, 134.50, 157.98, 163.38. ES-MS m/z 554 (M+H). Anal. Calcd. for C32H36N7OF.0.2CH2Cl2: C, 67.77; H, 6.43; N, 17.18; F, 3.33. Found: C, 68.16; H, 6.64; N, 16.86; F, 3.05.
出典と根拠
- ORDレコード
- ord-1f2fcc75804644e3b6f6f141e38304f7
- 出典データセット
- uspto-grants-2009_02
- 特許番号
- US07491735B2
関連ノート
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