1-(4-(bromomethyl)phenyl)-1H-1,2,4-triazole → 4-methyl-2-[1-(4-[1,2,4]triazol-1-yl-benzyl)-1H-pyrazol-3-yl]-thiazole-5-carboxylic acid (pyridin-3-ylmethyl)amide
Reaktionsgleichung
[N:1]1[CH:6]=[CH:5][CH:4]=[C:3]([CH2:7][NH:8][C:9]([C:11]2[S:15][C:14]([C:16]3[NH:17][N:18]=[CH:19][CH:20]=3)=[N:13][C:12]=2[CH3:21])=[O:10])[CH:2]=1.Br[CH2:23][C:24]1[CH:29]=[CH:28][C:27]([N:30]2[CH:34]=[N:33][CH:32]=[N:31]2)=[CH:26][CH:25]=1>>[N:1]1[CH:6]=[CH:5][CH:4]=[C:3]([CH2:7][NH:8][C:9]([C:11]2[S:15][C:14]([C:16]3[CH:20]=[CH:19][N:18]([CH2:23][C:24]4[CH:25]=[CH:26][C:27]([N:30]5[CH:34]=[N:33][CH:32]=[N:31]5)=[CH:28][CH:29]=4)[N:17]=3)=[N:13][C:12]=2[CH3:21])=[O:10])[CH:2]=1Komponenten
3
Versuchsvorschrift
The title compound was prepared from 4-methyl-2-(2H-pyrazol-3-yl)-thiazole-5-carboxylic acid (pyridin-3-ylmethyl)-amide and 1-(4-bromomethyl-phenyl)-1H-[1,2,4]-triazole as described in Example 49 and isolated as a white solid (76 mg, 51% yield). 1H NMR (400 MHz, CDCl3) δ 8.62 (s, 1H), 8.53-8.57 (m, 1H), 8.54 (s, 1H), 8.10 (s, 1H), 7.66-7.71 (m, 3H), 7.45 (bs, 1H), 7.39 (d, J=8 Hz, 1H), 7.37-7.41 (m, 1H), 6.88 (s, 1H), 6.05-6.12 (m, 1H), 5.41 (s, 2H), 4.63 (d, J=4 Hz, 2H), 2.75 (s, 3H); MS (M+H)+=457.2; Rt=1.08 min; HRMS (M+H)+=457.16.
Quellen und Nachweise
- ORD-Eintrag
- ord-2aaf06f720db40b1807dda9b40ca6cd1
- Quelldatensatz
- uspto-grants-2012_11
- Patentnummer
- US08314138B2
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