反应详情

A mixture of 0.2 g of trans-N-(4-{4-[benzyl((2S)-3-{4-(benzyloxy)-3-[(methylsulfonyl)-amino]phenoxy}-2-hydroxypropyl)amino]cyclohexyl}-benzoyl)-L-phenylalanine (0.248 mmol) and of 0.1 g of 10% palladium-on-charcoal (50% in water) in ethanol (15 ml) is placed under hydrogen atmosphere and stirred for 3 h. The reaction mixture is filtered through celite. The solvents are evaporated under reduced pressure and trans-N-(4-{4-[((2S)-2-hydroxy-3-{4-hydroxy-3-[(methylsulfonyl)amino]phenoxy}propyl)amino]cyclohexyl}benzoyl)-L-phenylalanine is obtained in the form of a white solid (0.049 g, 31%) after purification on C18-grafted silica (eluent: water/acetonitrile, 95/5 to 5/95 gradient in 15 min).

1. filtrationThe reaction mixture is filtered through celite
2. customThe solvents are evaporated under reduced pressure