Tert-butyl(+/-)-3-(3-{[{4-[(acetyloxy)methyl]phenyl}(cyclopentyl)-acetyl]amino}-2-methylphenyl)propanoate → tert-Butyl(+/-)-3-[3-({cyclopentyl[4-(hydroxymethyl)phenyl]acetyl}amino)-2-methylphenyl]propanoate

HRID 877190ノート

反応式

HRID 877190 の反応式
C([O:4][CH2:5][C:6]1[CH:11]=[CH:10][C:9]([CH:12]([CH:32]2[CH2:36][CH2:35][CH2:34][CH2:33]2)[C:13]([NH:15][C:16]2[C:17]([CH3:31])=[C:18]([CH2:22][CH2:23][C:24]([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25])[CH:19]=[CH:20][CH:21]=2)=[O:14])=[CH:8][CH:7]=1)(=O)C>N.CO>[CH:32]1([CH:12]([C:9]2[CH:10]=[CH:11][C:6]([CH2:5][OH:4])=[CH:7][CH:8]=2)[C:13]([NH:15][C:16]2[C:17]([CH3:31])=[C:18]([CH2:22][CH2:23][C:24]([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25])[CH:19]=[CH:20][CH:21]=2)=[O:14])[CH2:36][CH2:35][CH2:34][CH2:33]1

参加物

4

反応物 1

HCID 58136347Tert-butyl(+/-)-3-(3-{[{4-[(acetyloxy)methyl]phenyl}(cyclopentyl)-acetyl]amino}-2-methylphenyl)propanoate

生成物 1

HCID 58136762tert-Butyl(+/-)-3-[3-({cyclopentyl[4-(hydroxymethyl)phenyl]acetyl}amino)-2-methylphenyl]propanoate

試薬・触媒・溶媒 2

HCID 222Ammonia溶媒HCID 887Methanol溶媒

反応条件

温度
35 °C

実験手順

16.0 g (32.41 mmol) of tert-butyl(+/−)-3-(3-{[{4-[(acetyloxy)methyl]phenyl}(cyclopentyl)-acetyl]amino}-2-methylphenyl)propanoate were dissolved in 300 ml of a 2 M solution of ammonia in methanol and initially stirred at 30-40° C. for 2 h and then overnight at RT. The solution was then concentrated under reduced pressure and the residue was purified by chromatography on silica gel (mobile phase dichloromethane/methanol 100:1). This gave 13.6 g (93.1% of theory) of the title compound.

後処理

  1. customovernight
  2. customat RT
  3. concentrationThe solution was then concentrated under reduced pressure
  4. customthe residue was purified by chromatography on silica gel (mobile phase dichloromethane/methanol 100:1)

出典と根拠

ORDレコード
ord-ba0cebb5bb914556b274ee72d473c527
出典データセット
uspto-grants-2015_03
特許番号
US08987256B2

反応ノート

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