Cesium carbonate → 3-[2-Chloro-4-(4-chloro-2-fluoro-phenylamino)-benzoyl]-4-methyl-benzoic acid methyl ester

Participants

Reaction Conditions

Reaction Steps

1-Bromo-4-chloro-2-fluorobenzene (820 μL, 6.58 mmol) was dissolved in 20 mL dry 1,4-dioxane under an argon atmosphere. Compound 402 (2.00 g, 6.58 mmol) was added and dissolved in the solvent. Dicyclohexyl-(2′,4′,6′-triisopropyl-biphenyl-2-yl)-phosphane (125 mg, 0.26 mmol), Pd(OAc)2 (30 mg, 0.13 mmol) and Cs2CO3 (2.68 g, 8.22 mmol) were added, and the reaction mixture was stirred under an argon atmosphere at 120° C. for 48 h. The reaction mixture was filtered and then purified by flash chromatography using EtOAc/petroleum ether (40-60) 1:9 as the eluent to afford the title compound as a solid.

Provenance & Evidence