反应 #866

ord-b4a1a9f06c874053b3ad0f85aaa15884

反应方程式

CC[C@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)OCc1ccccc1)C(Cc1ccccc1)C(=O)O)[C@H](C)CC)c1ccccc1
N-benzyloxycarbonyl-β-benzyl-L-aspartyl-D-isoleucine (S)-α-ethylbenzylamide
CC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)[C@H](C)CC)c1ccccc1
α-L-aspartyl-D-isoleucine (S)-α-ethylbenzylamide
收率 72.3%

反应条件

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
  3. 3
    其他The crystals thus precipitated
  4. 4
    过滤were taken out by filtration
  5. 5
    其他dried

实验过程

To a suspension of 2.81 g (4.7 mmols) of N-benzyloxycarbonyl-β-benzyl-L-aspartyl-D-isoleucine (S)-α-ethylbenzylamide in 150 ml of methanol and 50 ml of water was added 2.0 g of 10% Pd-carbon (water content 50%). The mixture was reduced under hydrogen at room temperature for 5 hours. The catalyst was removed by filtration, and the resulting filtrate was concentrated under reduced pressure to be 20 ml. The crystals thus precipitated were taken out by filtration and dried to obtain 1.22 g (3.4 mmols) of α-L-aspartyl-D-isoleucine (S)-α-ethylbenzylamide.

来源

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