Morpholine → N-(5-chloro-2-fluorophenyl)-4-(1-hydroxy-2-morpholinoethyl)-N-isobutylbenzenesulfonamide

HRID 1487066ノート

反応式

HRID 1487066 の反応式
[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

  1. customThe mixture was then purified by mass
  2. 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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