反应详情

To a stirred solution of (RS)-2-(2,6-difluoro-3-phenylamino-phenyl)-N-[4-(N-hydroxycarbamimidoyl)-benzyl]-2-methoxy-acetamide (106 mg) at rt in ethanol (5 ml) under an argon atmosphere were added 5 drops of acetic acid and and a catalytic amount of Raney-Nickel. The mixture was then stirred at rt under a hydrogen atmosphere for 23 h. The catalyst was filtered off and the filtrate was concentrated. The crude product was purified using flash chromatography (EtOAc/acetone/H2O/HOAc 6:2:1:1) to give (RS)-N-(4-carbamimidoyl-benzyl)-2-(2,6-difluoro-3-phenylamino-phenyl)-2-methoxy-acetamide acetate (92 mg) as on off-white solid. MS 425.5 ([M+H]+)

1. filtrationThe catalyst was filtered off
2. concentrationthe filtrate was concentrated
3. customThe crude product was purified