反应详情

N-[6-(2-Benzyloxy-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide (100 mg, 0.202 mmol) was hydrogenated over 10% Pd/C in MeOH (5 mL) for 16 h at r.t. The catalyst was removed by filtration over Celite. The solution was concentrated in vacuo and the resulting resin was dissolved in DCM (1 mL). Hexanes (4 mL) was added and the precipitate was filtered off, washed with hexanes and dried to afford the title compound as a grey powder (66 mg, 81% yield). ES-MS: m/z 447.3 [M+CH3CN+H]+, rt 4.90 min. 1H-NMR (DMSO-d6, 400 MHz) 8.00 (s, H), 7.63 (s, 1H), 7.26 (d, J=2.34 Hz, 1H), 6.30 (d, J=1.89 Hz, 1H), 3.17 (s, 3H).

1. customThe catalyst was removed by filtration over Celite
2. concentrationThe solution was concentrated in vacuo
3. dissolutionthe resulting resin was dissolved in DCM (1 mL)
4. additionHexanes (4 mL) was added
5. filtrationthe precipitate was filtered off
6. washwashed with hexanes
7. customdried