Potassium Carbonate → 4-Fluoro-1-(4-fluoro-3-(pyrimidin-5-yl)phenyl)-1-(2-(trifluoromethyl)pyridin-4-yl)-1H-isoindol-3-amine

Participants

Reaction Conditions

Reaction Steps

1-(3-Bromo-4-fluorophenyl)-4-fluoro-1-(2-(trifluoromethyl)pyridin-4-yl)-1H-isoindol-3-amine (0.30 g, 0.64 mmol) and 5-pyrimidinylboronic acid (0.104 g, 0.84 mmol) in DMF (5.00 mL) was heated to 90° C. under argon atmosphere. Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium (II) dichloromethane adduct (0.039 g, 0.05 mmol) and aqueous potassium carbonate (2.00 M) (0.961 mL, 1.92 mmol) were added and the resulting mixture was stirred at 90° C. for 1 h. The reaction mixture was cooled to room temperature, and then filtered through a syringe filter and purified by preparative HPLC to give the title compound (0.158 g, 51% yield).

Provenance & Evidence