反応式
[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([O:42][CH:43]([F:45])[F:44])=[C:6]([C:8]2[C:12]([NH:13][C:14]([C:16]3[CH:17]=[N:18][N:19]4[CH:24]=[CH:23][CH:22]=[N:21][C:20]=34)=[O:15])=[CH:11][N:10]([CH2:25][C:26](=[O:41])[N:27]3[CH2:32][CH2:31][N:30]([CH:33]([C:35]4[CH:40]=CC=C[CH:36]=4)C)[CH2:29][CH2:28]3)[N:9]=2)[CH:7]=1.ClC1C=CC(OC(F)F)=C(C2C(NC(C3C=NN4C=CC=NC=34)=O)=CN(CC(O)=O)N=2)C=1.CC(C)CN1CCNCC1>>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([O:42][CH:43]([F:45])[F:44])=[C:6]([C:8]2[C:12]([NH:13][C:14]([C:16]3[CH:17]=[N:18][N:19]4[CH:24]=[CH:23][CH:22]=[N:21][C:20]=34)=[O:15])=[CH:11][N:10]([CH2:25][C:26]([N:27]3[CH2:28][CH2:29][N:30]([CH2:33][CH:35]([CH3:36])[CH3:40])[CH2:31][CH2:32]3)=[O:41])[N:9]=2)[CH:7]=1参加物
反応物 3
HCID 20520521-(2-Methylpropyl)piperazine
HCID 118522370{3-(5-Chloro-2-difluoromethoxy-phenyl)-4-[(pyrazolo[1,5-a]pyrimidine-3-carbonyl)amino]pyrazol-1-yl}acetic acid
HCID 118523141N-[3-[5-chloro-2-(difluoromethoxy)phenyl]-1-[2-oxo-2-[4-(1-phenylethyl)piperazin-1-yl]ethyl]-1H-pyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide生成物 1
実験手順
Using synthetic method analoguous to that of N-[3-[5-chloro-2-(difluoromethoxy)phenyl]-1-[2-oxo-2-[4-(1-phenylethyl)piperazin-1-yl]ethyl]-1H-pyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide, the title compound was prepared from {3-(5-Chloro-2-difluoromethoxyphenyl)-4-[(pyrazolo[1,5-a]pyrimidine-3-carbonyl)amino]pyrazol-1-yl}acetic acid and 1-(2-methylpropyl)piperazine. LCMS (Method 25) [M+H]+=587.1, RT=1.80 min. 1H NMR (300 MHz, DMSO-d6) δ: (ppm) 9.75 (s, 1H), 9.33 (dd, 1H, J=1.8, 6.9 Hz), 8.68 (dd, 1H, J=1.5, 3.9 Hz), 8.67 (s, 1H), 8.31 (s, 1H), 7.62 (dd, 1H, J=3.0, 8.7 Hz), 7.55 (d, 1H, J=2.7 Hz), 7.45 (d, 1H, J=9.0 Hz), 7.28 (dd, 1H, J=4.2, 7.2 Hz), 7.02 (t, 1H, J=73.2 Hz), 5.23 (s, 2H), 3.57-3.42 (m, 4H), 2.40-2.21 (m, 4H), 2.05 (d, 2H, J=7.2 Hz), 1.81-1.76 (m, 1H), 0.86 (d, 6H, J=6.3 Hz).
出典と根拠
- ORDレコード
- ord-828a622026de48efb15606da5f2e126c
- 出典データセット
- uspto-grants-2016_05
- 特許番号
- US09346815B2
関連ノート
読み込み中…