反应详情

Under an atmosphere of argon protective gas, benzyl {(7R)-6-cyano-7-(4-cyanophenyl)-5-methyl-4-[3-(trifluoromethyl)phenyl]-4,7-dihydro[1,2,4]triazolo[1,5-a]pyrimidin-2-yl}(methylsulfonyl)carbamate (16.0 mg, 11 μmol) was dissolved in degassed methanol (2 ml). After addition of a catalytic amount of palladium on activated carbon (10%), the mixture was hydrogenated under a hydrogen atmosphere (˜1 atm) at RT for 0.5 h. The reaction mixture was then filtered, the filtrate was concentrated under reduced pressure and the residue was purified by preparative HPLC (Gromsil C18 column, 30×250 mm; mobile phase: acetonitrile-water-0.1% TFA). After lyophilization, the product was obtained as a solid (8.5 mg, 71% of theory).

1. customat RT
2. customfor 0.5 h
3. filtrationThe reaction mixture was then filtered
4. concentrationthe filtrate was concentrated under reduced pressure
5. customthe residue was purified by preparative HPLC (Gromsil C18 column, 30×250 mm; mobile phase: acetonitrile-water-0.1% TFA)
6. customAfter lyophilization, the product was obtained as a solid (8.5 mg, 71% of theory)