Trifluoroacetic acid → (S)-5-((3-fluoropyrrolidin-1-yl)methyl)pyridin-2-amine
反応式
[F:1][C@H:2]1[CH2:6][CH2:5][N:4]([CH2:7][C:8]2[CH:9]=[CH:10][C:11]([NH:14]C(=O)OC(C)(C)C)=[N:12][CH:13]=2)[CH2:3]1.C(O)(C(F)(F)F)=O>ClCCl>[F:1][C@H:2]1[CH2:6][CH2:5][N:4]([CH2:7][C:8]2[CH:9]=[CH:10][C:11]([NH2:14])=[N:12][CH:13]=2)[CH2:3]1参加物
4
実験手順
To a solution of (S)-tert-butyl 5-((3-fluoropyrrolidin-1-yl)methyl)pyridin-2-ylcarbamate 119 (7.00 g, 23.7 mmol) in dichloromethane (70 mL) was added TFA (15.5 g, 142 mmol). The mixture was stirred for 12 h at room temperature. The solvent was removed in vacuo and sat. aq Na2CO3 was added. The mixture was extracted with dichloromethane, dried (MgSO4) and concentrated to give 120 (4.50 g, 97% yield).
後処理
- customThe solvent was removed in vacuo and sat. aq Na2CO3
- additionwas added
- extractionThe mixture was extracted with dichloromethane
- dry with materialdried (MgSO4)
- concentrationconcentrated
出典と根拠
- ORDレコード
- ord-0b63a8b1692447a6a669b542d9821e76
- 出典データセット
- uspto-grants-2016_05
- 特許番号
- US09326986B2
反応ノート
読み込み中…