Ammonium formate → 1-Azetidin-3-ylmethyl-6-fluoro-1H-indole
反応式
C([N:14]1[CH2:17][CH:16]([CH2:18][N:19]2[C:27]3[C:22](=[CH:23][CH:24]=[C:25]([F:28])[CH:26]=3)[CH:21]=[CH:20]2)[CH2:15]1)(C1C=CC=CC=1)C1C=CC=CC=1.C([O-])=O.[NH4+]>[Pd].C(O)C>[NH:14]1[CH2:17][CH:16]([CH2:18][N:19]2[C:27]3[C:22](=[CH:23][CH:24]=[C:25]([F:28])[CH:26]=3)[CH:21]=[CH:20]2)[CH2:15]1参加物
5
実験手順
A mixture of 1-(1-benzhydryl-azetidin-3-ylmethyl)-6-fluoro-1H-indole (0.6 g, 1.6 mmol), palladium on carbon (10%, cat.amount) and ammonium formate (0.2 g, 3.2 mmol) in ethanol (20 mL) was refluxed for 30 min. The mixture was filtered through celite and the solvent removed under vacuum. Diphenylmethane was removed by triturating the residue with ether, methylene chloride and decanting. The remaining product was dried under vacuum. The crude material was directly used in next step without further purification.
後処理
- temperaturewas refluxed for 30 min
- filtrationThe mixture was filtered through celite
- customthe solvent removed under vacuum
- customDiphenylmethane was removed
- customby triturating the residue with ether, methylene chloride
- customdecanting
- customThe remaining product was dried under vacuum
- customThe crude material was directly used in next step without further purification
出典と根拠
- ORDレコード
- ord-2821ea5e6cd14a7c971c8630357394c4
- 出典データセット
- uspto-grants-2008_09
- 特許番号
- US07419986B2
反応ノート
読み込み中…