反应详情

HCl (1.0 N in water, 2.09 mL) was added to a solution of the (2R)-4-[4-{4-[(6-methoxypyridin-3-yl)methoxy]phenyl}-2-oxopyridin-1(2H)-yl]-2-methyl-2-(methylsulfonyl)-N-(tetrahydro-2H-pyran-2-yloxy)butanamide (245 mg, 0.418 mmol) in IPA (5.0 mL) for 1 hour. The reaction mixture was concentrated and the residue was triturated with IPA to afford a white suspension at 50° C. for 30 minutes. A white solid was collected by filtration. Yield 215 mg/95% LCMS MS ES-500.1. 1H NMR (400 MHz, DMSO-d6) δ ppm 1.54 (s, 3 H) 2.07-2.23 (m, 1 H) 2.33-2.43 (m, 1 H) 3.08 (s, 3 H) 3.64-3.79 (m, 1 H) 3.83 (s, 3 H) 4.00-4.12 (m, 1 H) 5.09 (s, 3 H) 6.57-6.67 (m, 2 H) 6.80-6.88 (m, 1 H) 7.05-7.12 (m, 2 H) 7.64-7.73 (m, 3 H) 7.78 (s, 1 H) 8.26 (s, 1 H).

1. concentrationThe reaction mixture was concentrated
2. customthe residue was triturated with IPA
3. customto afford a white suspension at 50° C. for 30 minutes
4. filtrationA white solid was collected by filtration