反应详情

1,1-Dimethylethyl 4-({[4′-(methylsulfonyl)-4-biphenylyl]oxy}methyl)-1-piperidinecarboxylate (Example 1, 87 mg, 0.20 mmol) was dissolved in 1,4-dioxane (4 mL). Ether (3 mL) was added followed by addition of 4M HCl in 1,4-dioxane (3 mL) and 2M HCl in ether (3 mL). The reaction mixture was stirred at ambient temperature overnight. Ether (15 mL) was added, and the white solid was collected via filtration and washed with ether to yield 71 mg (95%) of 4-({[4′-(methylsulfonyl)-4-biphenylyl]oxy}methyl)piperidine hydrochloride as a white solid. 1H NMR (400 MHz, CD3OD): δ 7.98 (d, 2H, J=8.5 Hz), 7.83 (d, 2H, J=8.3 Hz), 7.66 (d, 2H, J=8.8 Hz), 7.05 (d, 2H, J=8.8 Hz), 3.97 (d, 2H, J=5.8 Hz), 3.50-3.40 (m, 2H), 3.13 (s, 3H), 3.10-3.00 (m, 2H), 2.25-2.05 (m, 3H), 1.70-1.55 (m, 2H); LRMS (ESI), m/z 346 (M+H).

1. filtrationthe white solid was collected via filtration
2. washwashed with ether