反应详情

温度

60 °C

In a 8-mL screw-cap vial, 4-amino-6-trifluoromethylpyrimidine (170 mg, 1.04 mmol) was added to a slurry of 1,1′-carbonyldiimidazole (169 mg, 1.04 mmol) in dichloroethane (0.35 mL). The mixture was heated at 60° C. for 30 hours. 4-(4Amino-3-fluoro-phenoxy)-pyridine-2-carboxylic acid methylamide (170 mg, 1.04 mmol) was then added and the mixture was heated overnight at to 60° C. The solvent was evaporated under reduced pressure, and the solid residue was washed with methanol to give the title product as a white solid (139 mg, yield 30%). 1H NMR (400 MHz, DMSO-d6) δ 10.6 (s, 1 H), 9.7 (s, 1 H), 9.0 (s, 1 H), 8.8 (s, 1 H), 8.5 (d, 1 H), 8.20 (m, 2 H), 7.40 (m, 2 H), 7.18 (d, 1 H), 7.10 (d, 1 H), 2.80 (s, 3 H). LC-MS m/z 451.3 [M+H]+.

1. customIn a 8-mL screw-cap vial
2. temperaturethe mixture was heated overnight at to 60° C
3. customThe solvent was evaporated under reduced pressure
4. washthe solid residue was washed with methanol