N-benzyloxycarbonyl-beta-benzyl-L-aspartyl-D-isoleucine (S)-alpha-ethylbenzylamide → alpha-L-aspartyl-D-isoleucine (S)-alpha-ethylbenzylamide

HRID 770

反应方程式

HRID 770 反应方程式
[CH2:1]([C@H:3]([NH:10][C:11](=[O:43])[C@@H:12]([C@@H:39]([CH2:41][CH3:42])[CH3:40])[NH:13][C:14](=[O:38])[C@H:15]([CH:27](CC1C=CC=CC=1)[C:28](=[O:30])[OH:29])[NH:16]C(OCC1C=CC=CC=1)=O)[C:4]1[CH:9]=[CH:8][CH:7]=[CH:6][CH:5]=1)[CH3:2]>CO.O.[Pd].[C]>[CH2:1]([C@H:3]([NH:10][C:11](=[O:43])[C@@H:12]([C@@H:39]([CH2:41][CH3:42])[CH3:40])[NH:13][C:14](=[O:38])[C@H:15]([CH2:27][C:28](=[O:29])[OH:30])[NH2:16])[C:4]1[CH:5]=[CH:6][CH:7]=[CH:8][CH:9]=1)[CH3:2]

参与物

5

反应物 1

HCID 53679369N-benzyloxycarbonyl-beta-benzyl-L-aspartyl-D-isoleucine (S)-alpha-ethylbenzylamide

产物 1

HCID 54262672alpha-L-aspartyl-D-isoleucine (S)-alpha-ethylbenzylamide收率 72.3%

试剂、催化剂与溶剂 3

HCID 178418390HCID 178418390，化合物催化剂HCID 887(5BETA,17BETA)-17-羟基-17-(甲基-D3)-2'H-雄甾-2-烯并[3,2-C]吡唑-5'(1'H)-酮溶剂HCID 962聚[6-[4-(4-氰基苯基)苯氧基]己基甲基丙烯酸酯]溶剂

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.

后处理

  1. customThe catalyst was removed by filtration
  2. concentrationthe resulting filtrate was concentrated under reduced pressure
  3. customThe crystals thus precipitated
  4. filtrationwere taken out by filtration
  5. customdried

来源与证据

ORD记录
ord-b4a1a9f06c874053b3ad0f85aaa15884
来源数据集
uspto-grants-1998_03
专利号
US05723165

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