Hydrogen chloride-ethyl acetate → N-((2S)-1-((2-(4-(benzyloxy)-3-fluorophenyl)[1,3]oxazolo[4,5-c]pyridin-6-yl)oxy)propan-2-yl)acetamide
反応式
[CH2:1]([O:8][C:9]1[CH:14]=[CH:13][C:12]([C:15]2[O:16][C:17]3[CH:22]=[C:21]([O:23][CH2:24][C@@H:25]([NH:27]C(=O)OC(C)(C)C)[CH3:26])[N:20]=[CH:19][C:18]=3[N:35]=2)=[CH:11][C:10]=1[F:36])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.Cl.[C:38](OCC)(=[O:40])[CH3:39]>>[CH2:1]([O:8][C:9]1[CH:14]=[CH:13][C:12]([C:15]2[O:16][C:17]3[CH:22]=[C:21]([O:23][CH2:24][C@@H:25]([NH:27][C:38](=[O:40])[CH3:39])[CH3:26])[N:20]=[CH:19][C:18]=3[N:35]=2)=[CH:11][C:10]=1[F:36])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1参加物
3
実験手順
To tert-butyl ((2S)-1-((2-(4-(benzyloxy)-3-fluorophenyl)[1,3]oxazolo[4,5-c]pyridin-6-yl)oxy)propan-2-yl)carbamate (1.72 g) was added 4 M hydrogen chloride/ethyl acetate (5 mL), and the mixture was stirred at room temperature for 10 min, and concentrated. To the residue were added pyridine (5 mL) and acetic anhydride (5 mL), and the mixture was stirred at room temperature for 15 min. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (NH, hexane/ethyl acetate) to give the title compound (1.21 g).
後処理
- concentrationconcentrated
- additionTo the residue were added pyridine (5 mL) and acetic anhydride (5 mL)
- stirringthe mixture was stirred at room temperature for 15 min
- concentrationThe reaction mixture was concentrated under reduced pressure
- customthe residue was purified by silica gel column chromatography (NH, hexane/ethyl acetate)
出典と根拠
- ORDレコード
- ord-358d870bc5b7496baed6226b254b0ed8
- 出典データセット
- uspto-grants-2015_09
- 特許番号
- US09133129B2
反応ノート
読み込み中…