反应详情

A solution of 1-(9-methyl-5,7,8,9-tetrahydro-6H-pyrido[3′,4′:4,5]pyrrolo[2,3-b]pyridin-2-yl)-4-(6-(trifluoromethyl)pyridin-3-yl)pyridin-2(1H)-one (0.49 g, 1.2 mmol) in MeOH (4.0 mL) was treated with 1.25 M HCl in MeOH (0.92 mL, 1.2 mmol), and the resulting suspension was stirred at ambient temperature for 4 h. The suspension was diluted with Et2O (50 mL) the resulting solids were collected by filtration, washed with CH2Cl2 (60 mL), and Et2O to provide the title compound (0.30 g, 55%) as a yellow powder: 307-316° C. decomp.; 1H NMR (500 MHz, DMSO-d6) δ 9.38 (s, 2H), 9.21 (d, J=2.5 Hz, 1H), 8.51 (dd, J=8.0, 2.0 Hz, 1H), 8.12 (d, J=8.5 Hz, 1H), 8.09-8.04 (m, 2H), 7.46 (d, J=8.0 Hz, 1H), 7.04 (d, J=2.0 Hz, 1H), 6.86 (dd, J=7.5, 2.0 Hz, 1H), 4.37 (s, 2H), 3.74 (s, 3H), 3.55 (t, J=6.5 Hz, 2H), 3.15 (t, J=6.0 Hz, 2H); ESI MS m/z 426 [M+H]+; HPLC (Method A)>99% (AUC), tR=13.1 min.

1. filtrationwere collected by filtration
2. washwashed with CH2Cl2 (60 mL), and Et2O