[NH2:1][C:2]1[C:3]([Br:20])=[CH:4][C:5]2[C:9]([CH:10]=1)=[N:8][N:7]([C:11]1[CH:16]=[CH:15][C:14]([F:17])=[CH:13][CH:12]=1)[C:6]=2[C:18]#N.[OH2:21].Cl.[OH-:23].[Na+]>>[NH2:1][C:2]1[C:3]([Br:20])=[CH:4][C:5]2[C:9]([CH:10]=1)=[N:8][N:7]([C:11]1[CH:16]=[CH:15][C:14]([F:17])=[CH:13][CH:12]=1)[C:6]=2[C:18]([OH:23])=[O:21]A suspension of 6-amino-5-bromo-2-(4-fluorophenyl)-2H-indazole-3-carbonitrile (50 mg, 0.14 mmol) in 10% NaOH (5 mL) was heated at 100° C. for 48 h. The reaction mixture was cooled to RT and poured into water (10 mL). After pH was adjusted to 4 with 1 N HCl, the mixture was extracted with EtOAc. The combined organic phases were washed with brine, dried over Na2SO4, filtered and evaporated to get 6-amino-5-bromo-2-(4-fluorophenyl)-2H-indazole-3-carboxylic acid (45 mg, yield: 85%). 1H-NMR (DMSO-d6, 400 MHz) δ 8.20 (s, 1H), 7.77˜7.82 (m, 2H), 7.45˜7.52 (m, 2H), 7.03 (s, 1H), 6.61 (s, 1H), 5.60 (s, 2H). MS (M+H)+: 350/352.
불러오는 중…
