反应详情

A mixture of 2-trifluoromethanesulfonyloxy-5-pyridinecarboxylic acid (0.442 g, 1.72 mmol), 2-thienylboronic acid (1.56 g, 12.79 mmol), barium hydroxide (0.813 mg, 2.58 mmol), DME (8 mL) and water (1.5 mL) is purged with dry argon. Tetrakis(triphenylphosphine) palladium(0) (99.0 mg, 0.086 mmol) is added, and the resultant solution is stirred at 80° C. for 4 hours. The solvents are evaporated in vacuo, and the residue is partitioned between EtOAc and water. The aqueous extract is separated, and extracted with EtOAc. The organic extracts are combined, washed with sat. aq. NaHCO3 and 5% aq. Na2S2O3, dried, (Na2SO4) and the solvent is evaporated in vacuo. The residue is purified by chromatography to afford the title compound.

1. customis purged with dry argon
2. customThe solvents are evaporated in vacuo
3. customthe residue is partitioned between EtOAc and water
4. extractionThe aqueous extract
5. customis separated
6. extractionextracted with EtOAc
7. washwashed with sat. aq. NaHCO3 and 5% aq. Na2S2O3
8. customdried
9. custom(Na2SO4) and the solvent is evaporated in vacuo
10. customThe residue is purified by chromatography