反应详情

温度

150 °C

A mixture of 5-bromo-6-(3-fluorophenyl)pyrazin-2-amine (Preparation 1, 100 mg, 0.37 mmol), thiazole (0.06 mL, 0.88 mmol) and potassium acetate (54 mg, 0.56 mmol) in N,N-dimethylacetamide (1 mL) was degassed with argon. The catalyst Pd(PPh3)4 (23 mg, 0.02 mmol, 5 mol %) was added and degassing was repeated. The mixture was heated to 150° C. in a sealed tube and stirred overnight. The mixture was cooled and ethyl acetate and aqueous NH4Cl were added. The aqueous layer was extracted with ethyl acetate. The organic layer was dried and concentrated. The residue was purified by flash silica gel chromatography (hexanes/EtOAc 1:1) to give the title compound (15 mg, 15%) as a yellow solid.

1. customwas degassed with argon
2. customdegassing
3. temperatureThe mixture was cooled
4. additionethyl acetate and aqueous NH4Cl were added
5. extractionThe aqueous layer was extracted with ethyl acetate
6. customThe organic layer was dried
7. concentrationconcentrated
8. customThe residue was purified by flash silica gel chromatography (hexanes/EtOAc 1:1)