2-Fluoro-3-(trifluoromethyl)phenol → 3-(4-Fluorophenyl)-2-[2-fluoro-3-(trifluoromethyl)phenoxy]pyrido[3,2-d]pyrimidin-4(3H)-one

関与物質

反応条件

反応手順

A mixture of 2-chloro-3-(4-fluorophenyl)pyrido[3,2-d]pyrimidin-4(3H)-one (55 mg, 0.20 mmol) and 2-fluoro-3-trifluoromethylphenol (50 μl, 0.40 mmol) is heated to 140° C. for 18 hours. After cooling to RT, the crude mixture is purified by column chromatography (gradient from CH2Cl2 to 20% EtOAc/CH2Cl2) to give the title compound as a white solid. 1H NMR (400 MHz, DMSO-d6) 8.71 (1H, m), 7.83 (2H, m), 7.70 (4H, m), 7.45 (3H, m). MS (M+1): 420.07; RT=1.13 min.

情報源と証拠