反応 #870

ord-1b033c485fa54b2cb55a6e97a581a99c

反応方程式

COC[C@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)OCc1ccccc1)C(Cc1ccccc1)C(=O)O)C(C)C)c1ccccc1
N-benzyloxycarbonyl-β-benzyl-L-aspartyl-D-valine (R)-α-methoxymethylbenzylamide
COC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)c1ccccc1
α-L-aspartyl-D-valine (R)-α-methoxymethylbenzylamide
収率 70.1%

反応条件

温度
40°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他The catalyst was removed by filtration
  2. 2
    濃縮the resulting filtrate was concentrated under reduced pressure to 15 ml
  3. 3
    その他The crystal thus precipitated
  4. 4
    その他was removed by filtration
  5. 5
    その他dried

実験手順

To a suspension of 6.20 g (10.5 mmols) of N-benzyloxycarbonyl-β-benzyl-L-aspartyl-D-valine (R)-α-methoxymethylbenzylamide in 200 ml of methanol and 50 ml of water was added 1.50 g of 10% Pd-carbon (water content 50%). The mixture was reduced under hydrogen under heat at 40° C. The catalyst was removed by filtration, and the resulting filtrate was concentrated under reduced pressure to 15 ml. The crystal thus precipitated was removed by filtration and dried to obtain 2.69 g (7.36 mmols, 70.0% ) of α-L-aspartyl-D-valine (R)-α-methoxymethylbenzylamide.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US05723165uspto-grants-1998_03