5-Nitro-2-pyrrolidin-1-ylmethylbenzoxazole → 2-[(Pyrrolidin-1-yl)methyl]-1,3-benzoxazol-5-amine
反応式
[N+:1]([C:4]1[CH:5]=[CH:6][C:7]2[O:11][C:10]([CH2:12][N:13]3[CH2:17][CH2:16][CH2:15][CH2:14]3)=[N:9][C:8]=2[CH:18]=1)([O-])=O>[Pd].CCOC(C)=O.CO>[NH2:1][C:4]1[CH:5]=[CH:6][C:7]2[O:11][C:10]([CH2:12][N:13]3[CH2:14][CH2:15][CH2:16][CH2:17]3)=[N:9][C:8]=2[CH:18]=1参加物
4
実験手順
To a solution of 5-nitro-2-[(pyrrolidin-1-yl)methyl]benzoxazole (300 mg, 1.21 mmol) in a mixed solvent of EtOAc-MeOH (1:1, 70 mL) was added 10% Pd—C (40 mg), the flask was purged with argon, then the argon was replaced with H2, the reaction mixture was stirred under H2 atmosphere for 30 min. After filtration through Celite, washed with ethyl acetate. The solvents were evaporated to provide 263 mg (100%) of 5-amino-2-[(pyrrolidin-1-yl)methyl]benzoxazole as a yellow solid.
後処理
- customthe flask was purged with argon
- filtrationAfter filtration through Celite
- washwashed with ethyl acetate
- customThe solvents were evaporated
出典と根拠
- ORDレコード
- ord-0520fc1cf16541708cae4208b71cde02
- 出典データセット
- uspto-grants-2014_08
- 特許番号
- US08796259B2
反応ノート
読み込み中…