(E)-3-(3-(5-amino-3-(2-fluorophenyl)-1H-pyrazol-1-yl)phenyl)-2-methylacrylamide → 3-(3-(5-amino-3-(2-fluorophenyl)-1H-pyrazol-1-yl)phenyl)-2-methylpropanamide

HRID 1696592ノート

反応式

HRID 1696592 の反応式
[NH2:1][C:2]1[N:6]([C:7]2[CH:8]=[C:9](/[CH:13]=[C:14](\[CH3:18])/[C:15]([NH2:17])=[O:16])[CH:10]=[CH:11][CH:12]=2)[N:5]=[C:4]([C:19]2[CH:24]=[CH:23][CH:22]=[CH:21][C:20]=2[F:25])[CH:3]=1>CO.[Pd]>[NH2:1][C:2]1[N:6]([C:7]2[CH:8]=[C:9]([CH2:13][CH:14]([CH3:18])[C:15]([NH2:17])=[O:16])[CH:10]=[CH:11][CH:12]=2)[N:5]=[C:4]([C:19]2[CH:24]=[CH:23][CH:22]=[CH:21][C:20]=2[F:25])[CH:3]=1

参加物

4

反応物 1

HCID 67270652(E)-3-(3-(5-amino-3-(2-fluorophenyl)-1H-pyrazol-1-yl)phenyl)-2-methylacrylamide

生成物 1

HCID 672704203-(3-(5-amino-3-(2-fluorophenyl)-1H-pyrazol-1-yl)phenyl)-2-methylpropanamide収率 58%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 887Methanol溶媒

実験手順

(E)-3-(3-(5-amino-3-(2-fluorophenyl)-1H-pyrazol-1-yl)phenyl)-2-methylacrylamide (0.4192 g, 1.25 mmol, 1.00 eq) was hydrogenated (3.5 atm) over 10% Pd/C (0.0838 g, 0.0394 mmol, 0.0316 eq) in MeOH (5 ml) at RT for 36 h. Filtration through Celite® and evaporation yielded 0.245 g (58%) of crude 3-(3-(5-amino-3-(2-fluorophenyl)-1H-pyrazol-1-yl)phenyl)-2-methylpropanamide which was used as is in the next reaction. MS (ESI) m/z: 339.2 (M+H+).

後処理

  1. customat RT
  2. customfor 36 h
  3. filtrationFiltration
  4. customthrough Celite® and evaporation

出典と根拠

ORDレコード
ord-2d9b06d0aa18497b830e52e4a4bb790f
出典データセット
uspto-grants-2012_04
特許番号
US08163756B2

反応ノート

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