反应 #870

ord-1b033c485fa54b2cb55a6e97a581a99c

反应方程式

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
收率 70.1%

反应条件

温度
40°CELSIUS
详细条件
See reaction.notes.procedure_details.

后处理

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

实验过程

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.

来源

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