Morpholine → N-(5-chloro-2-fluorophenyl)-4-(1-hydroxy-2-morpholinoethyl)-N-isobutylbenzenesulfonamide
反応式
[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([F:25])=[C:6]([N:8]([CH2:21][CH:22]([CH3:24])[CH3:23])[S:9]([C:12]2[CH:17]=[CH:16][C:15]([CH:18]3[CH2:20][O:19]3)=[CH:14][CH:13]=2)(=[O:11])=[O:10])[CH:7]=1.[NH:26]1[CH2:31][CH2:30][O:29][CH2:28][CH2:27]1>C(O)C>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([F:25])=[C:6]([N:8]([CH2:21][CH:22]([CH3:24])[CH3:23])[S:9]([C:12]2[CH:17]=[CH:16][C:15]([CH:18]([OH:19])[CH2:20][N:26]3[CH2:31][CH2:30][O:29][CH2:28][CH2:27]3)=[CH:14][CH:13]=2)(=[O:10])=[O:11])[CH:7]=1参加物
4
反応条件
- 温度
- 50 °C
実験手順
To a stirred solution of N-(5-chloro-2-fluorophenyl)-N-isobutyl-4-(oxiran-2-yl)benzenesulfonamide (200 mg, 0.521 mmol) in ethanol (2 mL) at 25° C. was added morpholine (0.045 ml, 0.521 mmol) and the reaction mixture stirred at 50° C. for 24 hours. The mixture was then purified by mass directed autoprep (ammonium carbonate modifier). The appropriate fractions were combined and evaporated in vacuo to give the required product, 51.4 mg. LCMS [LCMS2] Rt 1.25 min, m/z (ES+) 471 (M+H).
後処理
- customThe mixture was then purified by mass
- customevaporated in vacuo
出典と根拠
- ORDレコード
- ord-e504f2459d394d45b64471836712f15a
- 出典データセット
- uspto-grants-2016_08
- 特許番号
- US09428452B2
反応ノート
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