反应详情

温度

100 °C

To an ambient temperature solution of 6-chloro-nicotinic acid methyl ester (12.4 g, 72 mmol) and 4-(trifluoromethyl)phenylboronic acid (15 g, 79 mmol) in dioxane (270 mL) is added CsF (38.3 g, 252 mmol) and the reaction mixture is degassed with nitrogen. PdCl2(dppf) (1.5 g) is added and the reaction mixture is heated to 100° C. over weekend. The reaction mixture was diluted with ethyl acetate, filtered through celite. The filtrate is concentrated. Purification of the crude product by column on silica gel (hexanes/ethyl acetate) gives 6-(4-trifluoromethyl-phenyl)-nicotinic acid methyl ester (18.3 g, 82.3% yield).

1. customthe reaction mixture is degassed with nitrogen
2. additionPdCl2(dppf) (1.5 g) is added
3. additionThe reaction mixture was diluted with ethyl acetate
4. filtrationfiltered through celite
5. concentrationThe filtrate is concentrated
6. customPurification of the crude product by column on silica gel (hexanes/ethyl acetate)