反应详情

温度

120 °C

To a suspension of methyl 2-bromothiazole-4-carboxylate (500 mg, 2.16 mmol), 2,6-difluoro-4-hydroxyphenylboronic acid (2 equiv., 767 mg) and potassium fluoride (3.3 equiv., 414 mg) in tetrahydrofuran (10 mL) and water (1 mL) was added bis(tri-tert-butylphosphine)palladium(0) (0.1 equiv., 110 mg) and the mixture was heated to 120° C. for 15 min in the microwave reactor. After in vacuo concentration, the reaction mixture was purified by CombiFlash (0 to 100% EtOAc in heptane) to provide 241 mg of the title compound as a ˜1:1 mixture with methyl 2-bromothiazole-4-carboxylate, which was used directly without further purification.

1. concentrationAfter in vacuo concentration
2. customthe reaction mixture was purified by CombiFlash (0 to 100% EtOAc in heptane)