O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate → N-(3-Amino-2,4-dichloro-benzyl)-2-methyl-2-fluoro-propionamide

HRID 1189625ノート

反応式

HRID 1189625 の反応式
[F:1][C:2]([CH3:7])([CH3:6])[C:3](O)=[O:4].[NH2:8][C:9]1[C:10]([Cl:18])=[C:11]([CH:14]=[CH:15][C:16]=1[Cl:17])[CH2:12][NH2:13].CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.[B-](F)(F)(F)F>C1COCC1>[NH2:8][C:9]1[C:10]([Cl:18])=[C:11]([CH:14]=[CH:15][C:16]=1[Cl:17])[CH2:12][NH:13][C:3](=[O:4])[C:2]([CH3:7])([F:1])[CH3:6]

参加物

5

反応物 3

HCID 2733207O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborateHCID 27828282-Fluoro-2-methylpropanoic acidHCID 568399683-(Aminomethyl)-2,6-dichloroaniline

生成物 1

HCID 67957110N-(3-Amino-2,4-dichloro-benzyl)-2-methyl-2-fluoro-propionamide

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

A mixture of 2-fluoroisobutyric acid (555 mg, 5.2 mmol), 3-amino-2,4-dichloro-benzylamine (1.00 g, 5.2 mmol), TBTU (1.85 g, 5.8 mmol), TEA (1.82 mL, 13 mmol) and THF is stirred at rt overnight. The mixture is concentrated, stirred with sat. aq NaHCO3-solution and the resulting precipitate is collected by filtration, washed with water and dried.

後処理

  1. concentrationThe mixture is concentrated
  2. stirringstirred with sat. aq NaHCO3-solution
  3. filtrationthe resulting precipitate is collected by filtration
  4. washwashed with water
  5. customdried

出典と根拠

ORDレコード
ord-f299b01f2c1343d79873e57443087ce6
出典データセット
uspto-grants-2014_03
特許番号
US08674113B2

反応ノート

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