反应详情

A mixture of 5-bromo-2-iodopyrimidine (88) (1.50 g, 5.27 mmol), 4-(trifluoromethoxy)phenylboronic acid (44) (1.185 g, 5.75 mmol) and Na2CO3 (1.11 g, 10.5 mmol) in toluene (120 mL) and water (15 mL) was purged with N2. Pd(PPh3)4 (60 mg, 0.05 mmol) was added and the mixture was refluxed under N2 for 17.5 h, then partitioned between EtOAc and water. Column chromatography of the organic portion on silica gel (eluting with 4:1 hexanes/CH2Cl2) gave 5-bromo-2-[4-(trifluoromethoxy)phenyl]pyrimidine (89) (1.264 g, 75%) as a white solid: mp 107-108° C.; 1H NMR (CDCl3) δ 8.83 (s, 2H), 8.46 (d, J=9.0 Hz, 2H), 7.31 (d, J=9.0 Hz, 2H). APCI MS m/z 319, 321 [M+H]+.

1. customwas purged with N2
2. temperaturethe mixture was refluxed under N2 for 17.5 h
3. custompartitioned between EtOAc and water