反应详情

HCl/dioxane (4M, 2 mL) was added at 0° C. to a solution of (R)-tert-butyl (3-hydroxy-3-(3-((6-methylpyridin-2-yl)methoxy)phenyl)propyl)carbamate (200 mg, 0.54 mmol) in MeOH (3 mL) and the reaction mixture was stirred at room temperature for 2 h. The reaction mixture was concentrated under reduced pressure to give after purification by triturating in diethyl ether Example 12 hydrochloride as a white solid. Yield (0.15 g, 52%); 1H NMR (400 MHz, DMSO-d6) δ 7.92 (bs, 1H), 7.74 (bs, 3H), 7.47 (bs, 1H), 7.40 (bs, 1H), 7.28 (t, J=8.0 Hz, 1H), 7.02 (s, 1H), 6.95-6.90 (m, 2H), 5.20 (s, 2H), 4.68-4.65 (m, 1H), 2.84 (bs, 2H), 2.56 (s, 3H), 1.88-1.83 (m, 2H); MS: m/z 273.20 [M+H]+.

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. customto give
3. customafter purification
4. customby triturating in diethyl ether Example 12 hydrochloride as a white solid
5. customYield (0.15 g, 52%)