反应详情

温度

100 °C

7-bromo-4-methylsulfanylthieno[3,2-d]pyrimidine (270 mg, 1.03 mmol) was added to 1,4-dioxane (10 mL), and 2-(2-fluoro-4-methanesulfonyl-phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (1.5 eq), tetrakis(triphenylphosphine)palladium(0) (71 mg, 0.06 eq), 2N aqueous sodium carbonate (3.1 mL, 3 eq) were sequentially added thereto while stirring. The reaction mixture was degassed with Ar(g), heated to 100° C., and stirred at 100° C. for 4 hours. After completion of the reaction using sodium bicarbonate, the reaction mixture was extracted twice with ethyl acetate. The collected organic layer was dried over anhydrous magnesium sulfate, dried, and concentrated under reduced pressure to obtain a foamy residue. The residue was crystallized in the presence of diethyl ether to obtain the title compound as a yellowish solid.

1. additionwere sequentially added
2. customThe reaction mixture was degassed with Ar(g)
3. stirringstirred at 100° C. for 4 hours
4. extractionthe reaction mixture was extracted twice with ethyl acetate
5. dry with materialThe collected organic layer was dried over anhydrous magnesium sulfate
6. customdried
7. concentrationconcentrated under reduced pressure
8. customto obtain a foamy residue
9. customThe residue was crystallized in the presence of diethyl ether