反应详情

To a solution of 4-(4-fluoro-phenyl)-2-(2-methyl-pyrrolidin-1-yl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-carboxylic acid tert-butyl ester (0.193 g, 0.47 mmol) in Et2O (2 mL) was added 4 M HCl in dioxane (2.5 mL). After 16 h, the mixture was concentrated and the residue was triturated with Et2O to give the title compound (0.124 g, 76%) as a white solid. MS (ESI): mass calcd. for C18H21FN4, 312.4; m/z found, 313.4 [M+H]+. 1H NMR (DMSO-d6): 9.54 (m, 2H), 7.64 (dd, J=8.5, 5.5, 2H), 7.37 (t, J=8.8, 2H), 4.23-4.04 (m, 3H), 3.58-3.36 (m, 4H), 3.03-2.95 (m, 2H), 2.08-1.96 (m, 2H), 1.93-1.85 (m, 1H), 1.71-1.64 (m, 1H), 1.21 (d, J=6.3, 3H).

1. concentrationthe mixture was concentrated
2. customthe residue was triturated with Et2O