Morpholine → 3-Bromo-4-fluoro-5-(morpholine-4-sulfonyl)-benzoic acid
反応式
[Br:1][C:2]1[CH:3]=[C:4]([CH:8]=[C:9]([S:12](Cl)(=[O:14])=[O:13])[C:10]=1[F:11])[C:5]([OH:7])=[O:6].CCN(C(C)C)C(C)C.[NH:25]1[CH2:30][CH2:29][O:28][CH2:27][CH2:26]1>O1CCOCC1.O.CCOC(C)=O>[Br:1][C:2]1[CH:3]=[C:4]([CH:8]=[C:9]([S:12]([N:25]2[CH2:30][CH2:29][O:28][CH2:27][CH2:26]2)(=[O:14])=[O:13])[C:10]=1[F:11])[C:5]([OH:7])=[O:6]参加物
6
実験手順
To a solution of 3-Bromo-5-chlorosulfonyl-4-fluoro-benzoic acid (3.0 g) in dioxane/water (9/1 (v/v), 30 ml) was added DiPEA (5 ml) and morpholine (1.65 ml). After stirring for 2 h, the mixture was diluted with EtOAc and washed with 2 M aq. HCl. The organic layer was dried (Na2SO4) and concentrated in vacuo. Yield: 2.6 g.
後処理
- washwashed with 2 M aq. HCl
- dry with materialThe organic layer was dried (Na2SO4)
- concentrationconcentrated in vacuo
出典と根拠
- ORDレコード
- ord-77b15367ff934c05ab679181d2efe732
- 出典データセット
- uspto-grants-2011_09
- 特許番号
- US08017782B2
反応ノート
読み込み中…