Water → Ethyl 3-(5-(2-(((2,4'-dichloro-2'-methyl-[1,1'-biphenyl]-4-yl)amino)methyl)-5-(trifluoromethyl)phenyl)picolinamido)propanoate

Beteiligte Stoffe

Reaktionsschritte

N-(2-bromo-4-(trifluoromethyl)benzyl)-2,4′-dichloro-2′-methyl-[1,1′-biphenyl]-4-amine (2.7 g, 5.5 mmol), ethyl 3-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)picolinamido)propanoate, prepared as in Step A above, (2.3 g, 6.6 mmol), Pd(dppf)Cl2 (452 mg, 0.6 mmol), and K2CO3 (1.5 g, 11.0 mmol) were dissolved in 1,4-dioxane (50 mL) and water (13 mL) and the resulting mixture was heated to 80° C. After 16 h the resulting mixture was cooled to room temperature, diluted with EtOAc, washed with water and brine, dried (Na2SO4), and dry packed onto silica gel. Column chromatography yielded the title compound.

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