反应详情

To a solution of (S)—N-(1-azabicyclo[2.2.2]oct-3-yl)-2-(1-methylcyclopropyl)benzoxazole-4-carboxamide (63 mg, 0.19 mmol) in methanol (2 mL) was added a solution of HCl in diethyl ether (1 N, 0.38 mL, 0.38 mmol) at room temperature slowly. The reaction mixture was diluted with diethyl ether. The resulting solid was filtered and washed with diethyl ether to afford (S)—N-(1-azabicyclo[2.2.2]oct-3-yl)-2-(1-methylcyclopropyl)benzoxazole-4-carboxamide hydrochloride (60 mg, 88%) as a white solid: 1H NMR (500 MHz, DMSO-d6) δ 10.22 (br s, 1H), 9.36 (d, J=6.6 Hz, 1H), 8.10 (d, J=8.0 Hz, 2H), 7.46 (t, J=7.9 Hz, 1H), 4.45-4.36 (m, 1H), 3.77-3.70 (m, 1H), 3.35-3.26 (m, 2H), 3.24 (t, J=7.9 Hz, 2H), 3.17 (dd, J=13.2, 3.7 Hz, 1H), 2.30-2.15 (m, 2H), 2.00-1.90 (m, 3H), 1.61 (s, 3H), 1.48-1.40 (m, 2H), 1.20-1.15 (m, 2H); MS (ESI+) m/z 326 (M+H); HPLC>99% (AUC), tR=11.65 min.

1. filtrationThe resulting solid was filtered
2. washwashed with diethyl ether