methyl (2S)-2-[[(1R)-1-(1-benzofuran-5-yl)-2-oxo-2-(2-phenylmethoxyanilino)ethyl]amino]-4-methylpentanoate → methyl N-{(1R)-1-(benzofuran-5-yl)-2-[(2-hydroxyphenyl)amino]-2-oxoethyl}-L-leucinate

HRID 2108706

反応式

HRID 2108706 の反応式
C([O:8][C:9]1[CH:14]=[CH:13][CH:12]=[CH:11][C:10]=1[NH:15][C:16](=[O:37])[C@H:17]([NH:27][C@H:28]([C:33]([O:35][CH3:36])=[O:34])[CH2:29][CH:30]([CH3:32])[CH3:31])[C:18]1[CH:19]=[CH:20][C:21]2[O:25][CH:24]=[CH:23][C:22]=2[CH:26]=1)C1C=CC=CC=1>[Pd].C(OCC)(=O)C>[O:25]1[C:21]2[CH:20]=[CH:19][C:18]([C@@H:17]([NH:27][C@H:28]([C:33]([O:35][CH3:36])=[O:34])[CH2:29][CH:30]([CH3:31])[CH3:32])[C:16]([NH:15][C:10]3[CH:11]=[CH:12][CH:13]=[CH:14][C:9]=3[OH:8])=[O:37])=[CH:26][C:22]=2[CH:23]=[CH:24]1

参加物

4

反応物 1

HCID 45076860methyl (2S)-2-[[(1R)-1-(1-benzofuran-5-yl)-2-oxo-2-(2-phenylmethoxyanilino)ethyl]amino]-4-methylpentanoate

生成物 1

HCID 45076859methyl N-{(1R)-1-(benzofuran-5-yl)-2-[(2-hydroxyphenyl)amino]-2-oxoethyl}-L-leucinate収率 82%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 8857Ethyl Acetate溶媒

実験手順

A mixture of palladium on carbon (10%, 500 mg), methyl N-[(1R)-2-{[2-(benzyloxy)phenyl]amino}-1-(benzofuran-5-yl)-2-oxoethyl]-L-leucinate (5.1 g) and ethyl acetate (60 ml) was stirred under a hydrogen atmosphere for 5 hours. The reaction was then filtered through Celite and the filter pad was washed with further portions of ethyl acetate. The combined organic fractions were evaporated to give methyl N-{(1R)-1-(benzofuran-5-yl)-2-[(2-hydroxyphenyl)amino]-2-oxoethyl}-L-leucinate (3.429 g).

後処理

  1. filtrationThe reaction was then filtered through Celite
  2. washthe filter pad was washed with further portions of ethyl acetate
  3. customThe combined organic fractions were evaporated

出典と根拠

ORDレコード
ord-2101ddd77f0040e1ac5433ee1c280240
出典データセット
uspto-grants-2009_04
特許番号
US07514437B2

関連ノート

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