Hydrogen chloride-ethyl acetate → (trans)-3-Azido-4-fluoropyrrolidine
反応式
[N:1]([C@H:4]1[C@H:8]([F:9])[CH2:7][N:6](C(OC(C)(C)C)=O)[CH2:5]1)=[N+:2]=[N-:3].Cl.CCOC(C)=O>CCOC(C)=O>[N:1]([C@H:4]1[C@H:8]([F:9])[CH2:7][NH:6][CH2:5]1)=[N+:2]=[N-:3]参加物
4
実験手順
To a solution of (trans)-tert-butyl 3-azido-4-fluoropyrrolidine-1-carboxylate (25 g, 109 mmol), as prepared in step 3 of Preparation 3, in EtOAc (100 mL) was added HCl/EtOAc (50 mL) at 0-5° C. Then the mixture was stirred at rt for 4 hr. The solid was filtered and washed with petroleum ether/EtOAc (2:1, 40 mL) to give the title compound (18 g) as a gray solid, which was used directly in the next step.
後処理
- filtrationThe solid was filtered
- washwashed with petroleum ether/EtOAc (2:1, 40 mL)
出典と根拠
- ORDレコード
- ord-c2d5c72fecf14a468acaea2a772f3814
- 出典データセット
- uspto-grants-2016_03
- 特許番号
- US09290496B2
反応ノート
読み込み中…