反应详情

温度

85 °C

To 3-methyl-4-trifluoromethanesulfonyloxy-benzofuran-2-carboxylic acid tert-butyl ester (285 mg, 0.75 mmol) in 3 mL of 1,2-dimethoxyethane was added K2CO3 (363 mg, 3.5 eq), pyridine-3-boronic acid (138 mg, 1.13 mmol), Pd(Ph3)4 (43 mg, 0.05 eq), and 0.5 mL of water. The mixture was heated and stirred in an 85° C. oil bath for 3 h. The reaction mixture was poured into water and was extracted with ethyl acetate. The organic extract was washed with water and dried over sodium sulfate. Removal of the solvent in vacuo gave the crude product, which was purified by column chromatography to give 202 mg of 3-methyl-4-pyridin-3-yl-benzofuran-2-carboxylic acid tert-butyl ester, obtained as white solid.

1. temperatureThe mixture was heated
2. extractionwas extracted with ethyl acetate
3. extractionThe organic extract
4. washwas washed with water
5. dry with materialdried over sodium sulfate
6. customRemoval of the solvent in vacuo
7. customgave the crude product, which
8. customwas purified by column chromatography