反応式
[CH:1]1([CH2:6][C@H:7]([CH2:34][N:35]([CH:44]=[O:45])[O:36]CC2C=CC=CC=2)[C:8]([N:10]2[C@H:14]([C:15]([NH:17][C:18]3[CH:23]=[CH:22][N:21]=[CH:20][N:19]=3)=[O:16])[CH2:13][CH2:12][N:11]2C(OCC2C=CC=CC=2)=O)=[O:9])[CH2:5][CH2:4][CH2:3][CH2:2]1>[OH-].[OH-].[Pd+2].CO>[CH:1]1([CH2:6][C@H:7]([CH2:34][N:35]([CH:44]=[O:45])[OH:36])[C:8]([N:10]2[C@H:14]([C:15]([NH:17][C:18]3[CH:23]=[CH:22][N:21]=[CH:20][N:19]=3)=[O:16])[CH2:13][CH2:12][NH:11]2)=[O:9])[CH2:2][CH2:3][CH2:4][CH2:5]1参加物
4
反応物 1
生成物 1
試薬・触媒・溶媒 2
実験手順
A mixture of phenylmethyl (3S)-2-[(2R)-3-cyclopentyl-2-({formyl[(phenylmethyl)oxy]amino}methyl)propanoyl]-3-[(4-pyrimidinylamino)carbonyl]-1-pyrazolidinecarboxylate (1.21 g, 1.96 mmol) and Pearlman's catalyst (0.276 g, 0.39 mmol) in methanol (109 ml) was degassed and placed under 1 atm of H2 at 25° C. After 2 hrs, the reaction mixture was filtered and concentrated. Purification by reverse phase HPLC (Gilson) provided (3S)-2-((2R)-3-cyclopentyl-2-{[formyl(hydroxy)amino]methyl}propanoyl)-N-4-pyrimidinyl-3-pyrazolidinecarboxamide (554 mg, 70% yield).
後処理
- customwas degassed
- customplaced under 1 atm of H2 at 25° C
- filtrationthe reaction mixture was filtered
- concentrationconcentrated
- customPurification by reverse phase HPLC (Gilson)
出典と根拠
- ORDレコード
- ord-f67dea67b5254abf83ab7e4dbdd92063
- 出典データセット
- uspto-grants-2014_12
- 特許番号
- US08901119B2
関連ノート
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