反应详情

N-[(3R,5R)-1-(Benzyloxy)-5-isopropyl-2-oxopyrrolidinyl]-N-propyl-4′-(trifluoromethyl)[1,1′-biphenyl]-4-sulfonamide (0.015 g, 0.026 mmoles, Example 28b) in 5.0 mL methanol was hydrogenated on 5% Pd/BaSO4 (0.005 g) at 1 atm H2 and 22° C. After 6 hours the solution was filtered through Celite and concentrated by rotary evaporation to afford 0.012 g (95% yield) of the title compound as a white solid. LC-MS (APCI) m/z 485 (M+1). 1H NMR (CD3OD) δ 8.07 (d, J=8 Hz, 2H), 7.89 (d, J=6 Hz, 2H), 7.87 (d, J=6 Hz, 2H), 7.79 (d, J=8 Hz, 2H), 4.69 (t, J=10 Hz, 1H), 3.57 (ddd, J1=4 Hz, J2=7 Hz, J3=10 Hz, 1H), 3.10 (t, J=8 Hz, 2H), 2.30–2.18 (m, 2H), 1.81–1.57 (m's, 3H), 0.95 (d, J=7 Hz, 3H), 0.90 (d, J=7 Hz, 3H) and 0.85 (t, J=8 Hz, 3H) ppm.

1. filtrationAfter 6 hours the solution was filtered through Celite
2. concentrationconcentrated by rotary evaporation