Methanol → 4-Fluoro-2-(morpholine-4-sulfonyl)-phenol

HRID 1971835

反応式

HRID 1971835 の反応式
[F:1][C:2]1[CH:3]=[CH:4][C:5]([O:17]C)=[C:6]([S:8]([N:11]2[CH2:16][CH2:15][O:14][CH2:13][CH2:12]2)(=[O:10])=[O:9])[CH:7]=1.BrB(Br)Br.CO>C(Cl)Cl>[F:1][C:2]1[CH:3]=[CH:4][C:5]([OH:17])=[C:6]([S:8]([N:11]2[CH2:12][CH2:13][O:14][CH2:15][CH2:16]2)(=[O:9])=[O:10])[CH:7]=1

参加物

5

反応物 3

HCID 887MethanolHCID 25134Boron tribromideHCID 8499944-(5-Fluoro-2-methoxy-benzenesulfonyl)-morpholine

生成物 1

HCID 581269904-Fluoro-2-(morpholine-4-sulfonyl)-phenol収率 90.8%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒2 回

実験手順

To a solution of 4-(5-fluoro-2-methoxyphenylsulfonyl)morpholine (0.5 g 1.8 mmol) in CH2Cl2 (10 ml) was added dropwise a solution of tribromoborane (0.593 mg 2.36 mmol) in CH2Cl2 (20 ml) at 0° C. The mixture was stirred at room temperature for 1 h, after which methanol (10 ml) was added to quench the reaction. The solvent was evaporated under reduced pressure and ethyl acetate (30 ml) was added, washed with water and then brine, dried and concentrated into dryness to give the product (427 mg, 90% yield).

後処理

  1. customto quench
  2. customthe reaction
  3. customThe solvent was evaporated under reduced pressure and ethyl acetate (30 ml)
  4. additionwas added
  5. washwashed with water
  6. dry with materialbrine, dried
  7. concentrationconcentrated into dryness

出典と根拠

ORDレコード
ord-ff47d3c2911042d6b8247f41505c199f
出典データセット
uspto-grants-2013_04
特許番号
US08431581B2

関連ノート

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