[NH2:1][C:2]([C:4]1[CH:8]=[C:7]([C:9]2[C:14]([F:15])=[CH:13][C:12]([C:16]([OH:19])([CH3:18])[CH3:17])=[CH:11][C:10]=2[F:20])[S:6][C:5]=1[NH:21][C:22]1[N:27]=[C:26]([CH2:28][N:29]2[CH:33]=[C:32]([C:34]([O:36]C)=[O:35])[N:31]=[N:30]2)[CH:25]=[CH:24][CH:23]=1)=[O:3].[OH-].[K+:39]>C1COCC1.CO>[NH2:1][C:2]([C:4]1[CH:8]=[C:7]([C:9]2[C:10]([F:20])=[CH:11][C:12]([C:16]([OH:19])([CH3:17])[CH3:18])=[CH:13][C:14]=2[F:15])[S:6][C:5]=1[NH:21][C:22]1[N:27]=[C:26]([CH2:28][N:29]2[CH:33]=[C:32]([C:34]([O-:36])=[O:35])[N:31]=[N:30]2)[CH:25]=[CH:24][CH:23]=1)=[O:3].[K+:39]Methyl 1-{[6-({3-(aminocarbonyl)-5-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-2-thienyl}amino)pyridin-2-yl]methyl}-1H-1,2,3-triazole-4-carboxylate (425 mg, 0.80 mmol) was taken up in THF (5.0 mL) and MeOH (5.0 mL), and KOH (1.0 M, 1.05 mL, 1.05 mmol) was added. The reaction was stirred at room temperature overnight. Additional KOH (1.0 M, 160 μL, 0.16 mmol) was added, and the reaction was stirred for another 8 h at room temperature. The mixture was then concentrated, resuspended in MeOH, and concentrated again to give the title compound as a yellow solid that was carried on without purification.
Wird geladen…