反应详情

5-Bromo-6-methoxy-nicotinic acid methyl ester (1.03 g, 4.18 mmol), 3-trifluoromethylbenzeneboronic acid (0.795 g, 4.19 mmol), tetrakis(triphenylphosphine)palladium(0) (24 mg, 0.021 mmol) and sodium bicarbonate (1.05 g, 12.5 mmol) were partitioned between toluene (10 ml) and water (10 ml) under argon and stirred in reflux for 1 h. The material was partitioned between ethyl acetate and water, the combined organic extracts were dried over sodium chloride, filtered over a small plug of silica and evaporated to dryness. The solid material was titured with methanol, filtered and dried in vacuo to yield the title compound (1.4 g) sufficiently pure for further synthesis.

1. temperaturein reflux for 1 h
2. customThe material was partitioned between ethyl acetate and water
3. dry with materialthe combined organic extracts were dried over sodium chloride
4. filtrationfiltered over a small plug of silica
5. customevaporated to dryness
6. filtrationfiltered
7. customdried in vacuo