反应详情

2-bromo-4-(trifluoromethyl)benzoic acid (538 mg, 2.0 mmol), ethyl 3-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)picolinamido)propanoate (1.0 g, 3.0 mmol), Pd(dppf)Cl2 (163 mg, 0.2 mmol), and K2CO3 (1.1 g, 8.0 mmol) were dissolved in 1,4-dioxane (12 mL) and water (4 mL) and heated to 90° C. After 3 h the resulting mixture was diluted EtOAc and water and 2N aqueous HCl was added until the pH of the aqueous layer was ca. 3-4. The layers were separated and the aqueous layer was extracted with EtOAc. The combined organic layers were dried (Na2SO4) and concentrated to yield the title compound, which was used in the next step without further purification.

1. customThe layers were separated
2. extractionthe aqueous layer was extracted with EtOAc
3. dry with materialThe combined organic layers were dried (Na2SO4)
4. concentrationconcentrated