tert-butyl ((1S,2S)-2-((5-(trifluoromethyl)-3-vinylpyrazin-2-yl)amino)cyclopentyl)carbamate → tert-butyl ((1S,2S)-2-((3-ethyl-5-(trifluoromethyl)pyrazin-2-yl)amino)cyclopentyl)carbamate

HRID 1750543ノート

反応式

HRID 1750543 の反応式
[CH:1]([C:3]1[C:4]([NH:13][C@H:14]2[CH2:18][CH2:17][CH2:16][C@@H:15]2[NH:19][C:20](=[O:26])[O:21][C:22]([CH3:25])([CH3:24])[CH3:23])=[N:5][CH:6]=[C:7]([C:9]([F:12])([F:11])[F:10])[N:8]=1)=[CH2:2].[H][H]>CO.[Pd]>[CH2:1]([C:3]1[C:4]([NH:13][C@H:14]2[CH2:18][CH2:17][CH2:16][C@@H:15]2[NH:19][C:20](=[O:26])[O:21][C:22]([CH3:25])([CH3:24])[CH3:23])=[N:5][CH:6]=[C:7]([C:9]([F:11])([F:10])[F:12])[N:8]=1)[CH3:2]

参加物

5

実験手順

To a solution of tert-butyl N-[(1S,2S)-2-{[3-ethenyl-5-(trifluoromethyl)pyrazin-2-yl]amino}cyclopentyl]carbamate (460 mg, 1.24 mmol) in methanol (12 ml) was added palladium on carbon (10% wt, 50% wet) (131 mg, 0.124 mmol) and the resulting mixture was stirred under a balloon of hydrogen gas for 2 hours. The reaction was filtered through diatomaceous earth (commercially sold under the trade mark “Celite”). To this was then added further palladium on carbon (10% wt, 50% wet) (131 mg, 0.124 mmol) and the resulting mixture was stirred under a balloon of hydrogen gas for 72 hours. The reaction was filtered through diatomaceous earth (commercially sold under the trade mark “Celite”) and concentrated in vacuo to afford the title compound.

後処理

  1. filtrationThe reaction was filtered through diatomaceous earth (
  2. additionTo this was then added further palladium on carbon (10% wt
  3. filtrationThe reaction was filtered through diatomaceous earth (
  4. concentrationconcentrated in vacuo

出典と根拠

ORDレコード
ord-d3de7360ee4b4da19541affa4c6937fc
出典データセット
uspto-grants-2015_10
特許番号
US09156829B2

反応ノート

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