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

Participants

Reaction Conditions

Reaction Steps

1-Bromo-3-fluoro-2-methyl-benzene (189 mg, 1.0 mmol) was dissolved in 4 mL dry 1,4-dioxane under an argon atmosphere. Compound 402 (304 mg, 1.00 mmol) was added and dissolved in the solvent. Dicyclohexyl-(2′,4′,6′-triisopropyl-biphenyl-2-yl)-phosphane (19 mg, 0.04 mmol), Pd(OAc)2 (5 mg, 0.02 mmol) and Cs2CO3 (407 mg, 1.25 mmol) were added, and the reaction mixture was stirred under an argon atmosphere at 120° C. for 60 h. The reaction mixture was filtered and then purified by flash chromatography using EtOAc/petroleum ether (40-60) 1:4 as the eluent to afford the title compound as a solid. 13C NMR (CDCl3) δ

Provenance & Evidence