Ethanolamine → tert-butyl (6R,7R)-7-(3,4-dichlorophenyl)-6-{[(2-hydroxyethyl)amino]methyl}-1,4-oxazepane-4-carboxylate
反応式
[Cl:1][C:2]1[CH:3]=[C:4]([C@@H:9]2[O:15][CH2:14][CH2:13][N:12]([C:16]([O:18][C:19]([CH3:22])([CH3:21])[CH3:20])=[O:17])[CH2:11][C@H:10]2COS(C)(=O)=O)[CH:5]=[CH:6][C:7]=1[Cl:8].[CH2:29]([CH2:31][NH2:32])[OH:30].[CH2:33](O)C>>[Cl:1][C:2]1[CH:3]=[C:4]([C@@H:9]2[O:15][CH2:14][CH2:13][N:12]([C:16]([O:18][C:19]([CH3:22])([CH3:20])[CH3:21])=[O:17])[CH2:11][C@H:10]2[CH2:33][NH:32][CH2:31][CH2:29][OH:30])[CH:5]=[CH:6][C:7]=1[Cl:8]参加物
4
反応条件
- 温度
- 80 °C
実験手順
To a solution of tert-butyl (6S,7R)-7-(3,4-dichlorophenyl)-6-{[(methylsulfonyl)oxy]methyl}-1,4-oxazepane-4-carboxylate (1.9 g) in ethanol (41.8 mL) was added ethanolamine (7.57 mL), and the mixture was stirred at 80° C. overnight. The reaction mixture was concentrated under reduced pressure, distilled water was added, and the mixture was extracted with ethyl acetate. The extract was washed with distilled water and brine, and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure to give the title compound (1.65 g).