反应详情

A suspension of 1-{3-[2-(7-benzyloxy-2-oxo-1,2-dihydroquinolin-5-yl)-2-hydroxyethylamino]-3-methylbutyl}-4,4-diethyl-1,4-dihydrobenzo[d][1,3]oxazin-2-one (152 mg, 0.338 mmol) and Pd/C (10%) (40 mg) in MeOH (12 mL) is hydrogenated at room temperature (RT) and 1 bar hydrogen pressure for 4 hours. The catalyst is filtered off through CELITE® filter aid and washed with MeOH (5 mL). The organic phase is evaporated down, the residue is triturated with EtOAc and the precipitate formed is filtered off and dried in vacuo. Yield: 76 mg (46%); Rf=0.3 (silica gel, dichloromethane/MeOH/saturated aqueous ammonia 90:10:0.5); ESI-MS: [M+H]+=494.

1. customis hydrogenated at room temperature
2. customfor 4 hours
3. filtrationThe catalyst is filtered off through CELITE®
4. filtrationfilter aid
5. washwashed with MeOH (5 mL)
6. customThe organic phase is evaporated down
7. customthe residue is triturated with EtOAc
8. customthe precipitate formed
9. filtrationis filtered off
10. customdried in vacuo