Dimethylformamide → HCID 49871953, compound

Participants

Reaction Steps

To a solution of 2-[1-(4,4-difluorocyclohexyl)piperidin-4-yl]-6-fluoro-1-methyl-3-oxo-2,3-dihydro-1H-isoindole-4-carboxylic acid hydrochloride (80 mg, 0.2 mmol) in N,N-dimethylformamide (2 mL) hydroxybenzotriazole ammonium salt (61 mg, 0.4 mmol), 1-ethyl-3-(3′-dimethylamino) carbodiimide hydrochloric acid salt (77 mg, 0.4 mmol) and N,N-diisopropylethylamine (0.14 mL, 1 mmol) were added. The reaction mixture was stirred at room temperature overnight. The solvent was removed under reduce pressure and the residue was dissolved in ethyl acetate. The solution was washed twice with sodium carbonate saturated aqueous solution, and the organic phase was dried over anhydrous sodium sulfate and concentrated in vacuo. The crude was purified by flash chromatography (dichloromethane/methanol 96:4) to afford the title compound (60 mg, 73%) as a white solid.

Provenance & Evidence