Tert-butyl (2S)-2-amino-3-[4-(tert-butoxy)phenyl]propanoate → 2-{2-[(Azepane-1-carbonyl)-amino]-4-methyl-pentanoylamino}-3-(4-tert-butoxy-phenyl)-propionic acid tert-butyl ester

HRID 2230303

反応式

HRID 2230303 の反応式
[N:1]1([C:8]([NH:10][C@@H:11]([CH2:15][CH:16]([CH3:18])[CH3:17])[C:12]([OH:14])=O)=[O:9])[CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2]1.[C:19]([O:23][C:24](=[O:39])[C@@H:25]([NH2:38])[CH2:26][C:27]1[CH:32]=[CH:31][C:30]([O:33][C:34]([CH3:37])([CH3:36])[CH3:35])=[CH:29][CH:28]=1)([CH3:22])([CH3:21])[CH3:20]>>[C:19]([O:23][C:24](=[O:39])[CH:25]([NH:38][C:12](=[O:14])[CH:11]([NH:10][C:8]([N:1]1[CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7]1)=[O:9])[CH2:15][CH:16]([CH3:18])[CH3:17])[CH2:26][C:27]1[CH:28]=[CH:29][C:30]([O:33][C:34]([CH3:37])([CH3:36])[CH3:35])=[CH:31][CH:32]=1)([CH3:20])([CH3:22])[CH3:21]

参加物

3

反応物 2

HCID 7350495Tert-butyl (2S)-2-amino-3-[4-(tert-butoxy)phenyl]propanoateHCID 7530182(2S)-2-(azepane-1-carbonylamino)-4-methylpentanoic acid

生成物 1

HCID 700602632-{2-[(Azepane-1-carbonyl)-amino]-4-methyl-pentanoylamino}-3-(4-tert-butoxy-phenyl)-propionic acid tert-butyl ester収率 29%

実験手順

A solution of the product from Example Z (2(S)-[(azepane-1-carbonyl)-amino]-4-methyl-pentanoic acid) (0.20 g, 0.78 mmol) and 2(S)-amino-3-(4-tert-butoxy-phenyl)-propionic acid tert-butyl ester (Bachem, 0.284 g, 0.86 mmol) were coupled according to the procedure described in Example 3. The residue was purified by chromatography (silica gel, 1:1 ethyl acetate/hexane) to give the title compound as a white solid (0.096 g, 29%), mp=87-90° C.

後処理

  1. customThe residue was purified by chromatography (silica gel, 1:1 ethyl acetate/hexane)

出典と根拠

ORDレコード
ord-4face217ff86433386e63654607f3135
出典データセット
uspto-grants-2002_07
特許番号
US06423689B1

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