Azepane → 3-[8-(2,6-difluorophenyl)-2-(hexahydro-1H-azepin-1-yl)-7-oxo-5,6,7,8-tetrahydropyrimido[4,5-d]pyrimidin-4-yl]-4-methyl-N-(1-methylethyl)benzamide

関与物質

反応手順

To a solution of compound 3-[8-(2,6-difluorophenyl)-2-(methylsulfinyl)-7-oxo-5,6,7,8-tetrahydropyrimido[4,5-d]pyrimidin-4-yl]-4-methyl-N-(1-methylethyl)benzamide (50 mg, 0.10 mmol) in DCM (5 mL) was added hexahydro-1H-azepine (0.034 mL, 0.30 mmol). The resultant solution was stirred at room temperature over night. The result mixture was concentrated. CombiFlash chromatography (mobile phase DCM/DCM [90]+MeOH[7]+NH4OH[3]) provided the title compound as a white solid (39 mg, 73%). LC-MS m/z 535 (M+H)+; 1H-NMR (MeOD) δ 1.27 (d, 6H), 1.47 (m, 6H), 1.70 (m, 2H), 2.31 (s, 3H), 3.32 (m, 2H), 3.68 (m, 2H), 4.11 (m, 2H), 4.23 (m, 1H), 7.13 (t, 2H), 7.44 (d, 1H), 7.48 (m, 1H), 7.69 (s, 1H), 7.85 (d, 1H).

情報源と証拠