Cesium carbonate → HCID 117801546, compound

Participants

Reaction Conditions

Reaction Steps

To a degassed solution of 7-bromo-2-(4-fluorobenzyl)isoquinolin-1(2H)-one (149 mg, 0.45 mmol) and 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide (150 mg, 0.30 mmol) in 1,4-dioxane (5 mL) and water (300 μl) was added Cs2CO3 (195 mg, 0.60 mmol) and 1,1′-bis(di-tert-butylphosphino)ferrocene palladium dichloride (19 mg, 0.03 mmol) under N2 protection. The resulting mixture was heated to 90° C. and stirred at this temperature for 3 h. The reaction was cooled, filtered through a pad of celite and washed with ethyl acetate. The combined filtrate was evaporated in vacuo. The resulting residue was purified using column chromatography (eluted with 0-30% EtOAc/DCM) to provide 5-(2-(4-fluorobenzyl)-1-oxo-1,2-dihydroisoquinolin-7-yl)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (140 mg, yield: 75%). (M+H)+: 628.

Provenance & Evidence