反应详情

温度

80 °C

N-(2-bromo-6-chloro-4-(trifluoromethyl)benzyl)-2′,4′-dichloro-[1,1′-biphenyl]-4-amine (4.5 g, 8.8 mmol) and ethyl 3-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)picolinamido)propanoate (3.1 g, 8.8 mmol), Pd(dppf)Cl2 (321 mg, 0.4 mmol), and 2 M K2CO3 (aq) (8.8 mL, 17.6 mmol) were dissolved in 1,4-dioxane (35 mL) and heated to 80° C. After 1 h the reaction was cooled to room temperature diluted with EtOAc and 4M aqueous NaCl, and the layers were separated. The aqueous layer was extracted with EtOAc and the combined organics were dried (Na2SO4), concentrated, and purified via column chromatography to yield the title compound.

1. temperatureAfter 1 h the reaction was cooled to room temperature
2. customthe layers were separated
3. extractionThe aqueous layer was extracted with EtOAc
4. dry with materialthe combined organics were dried (Na2SO4)
5. concentrationconcentrated
6. custompurified via column chromatography