5-Amino-4-fluoro-2-methylphenol → ZM 323881 hydrochloride
反応式
[F:1][C:2]1[CH:8]=[C:7]([CH3:9])[C:6]([OH:10])=[CH:5][C:3]=1[NH2:4].Cl.[CH2:12]([O:19][C:20]1[CH:29]=[C:28]2[C:23]([C:24]([Cl:30])=[N:25][CH:26]=[N:27]2)=[CH:22][CH:21]=1)[C:13]1[CH:18]=[CH:17][CH:16]=[CH:15][CH:14]=1>CC(O)CCC>[ClH:30].[CH2:12]([O:19][C:20]1[CH:29]=[C:28]2[C:23]([C:24]([NH:4][C:3]3[CH:5]=[C:6]([OH:10])[C:7]([CH3:9])=[CH:8][C:2]=3[F:1])=[N:25][CH:26]=[N:27]2)=[CH:22][CH:21]=1)[C:13]1[CH:14]=[CH:15][CH:16]=[CH:17][CH:18]=1参加物
4
反応条件
- 温度
- 120 °C
実験手順
2-Fluoro-5-hydroxy-4-methylaniline (170 mg, 1.2 mmol), (prepared as described for the starting material in Example 13), was added to a solution of 7-benzyloxy-4-chloroquinazoline hydrochloride (307 mg, 1 mmol) in 2-pentanol (5 ml) and the mixture stirred at 120° C. for 2 hours. The mixture was allowed to cool and the resulting precipitate was collected by filtration, washed with isopropanol and then ether and dried under vacuum at 70° C. to give 7-benzyloxy-4-(2-fluoro-5-hydroxy-4-methylanilino)quinazoline hydrochloride (331 mg, 80%).