反応式
[CH2:1]([N:8]1[CH:12]=[CH:11][N:10]=[C:9]1[C:13]1[CH:14]=[N:15][CH:16]=[CH:17][CH:18]=1)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[C:19]([C:21]1[CH:22]=[N:23][CH:24]=[CH:25][CH:26]=1)#[N:20].B(O)(O)[C:28]1[CH:33]=CC=[C:30](F)[CH:29]=1>ClCCl.CO>[C:25]1([C:24]2[N:20]=[CH:19][C:21]([C:12]3[NH:8][C:9]([C:13]4[CH:14]=[N:15][CH:16]=[CH:17][CH:18]=4)=[N:10][CH:11]=3)=[CH:22][N:23]=2)[CH:26]=[CH:30][CH:29]=[CH:28][CH:33]=1.[CH2:1]([N:8]1[CH:12]=[CH:11][N:10]=[C:9]1[C:13]1[CH:14]=[N:15][CH:16]=[CH:17][CH:18]=1)[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1参加物
6
実験手順
The title compound was prepared by the method described in Example 1, except that 3-(1-benzyl-1H-imidazol-2-yl)pyridine was used instead of 1-benzyl-2-phenyl-1H-imidazole in Step C. 3-(1-Benzyl-1H-imidazol-2-yl)pyridine was prepared by the method described in Example 8, Steps A and B except the commercially available 3-cyanopyridine was used instead of 3-fluorobenzonitrile; Rf 0.25 with 95:5 v/v dichloromethane-methanol; melting point 308° C; 1H-NMR (400 MHz; DMSO-d6) δ 9.32 (s, 2H), 9.20 (d, 1H), 8.58 (dd, 1H), 8.44-8.31 (m, 3H), 8.12 (m, 1H), 7.57-7.46 (m, 4H); MS (ESI+) m/z 300.1 (M+1); H-PGDS FPBA IC50: 0.079 μM; H-PGDS inhibitor EIA IC50: 0.021 μM.
出典と根拠
- ORDレコード
- ord-4d2fcb8da0d046818c6484d02419b0b8
- 出典データセット
- uspto-grants-2013_09
- 特許番号
- US08536185B2
関連ノート
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