Potassium Carbonate → HCID 57834979, compound

Participants

Reaction Conditions

Reaction Steps

4-Bromo-1-(3-fluoro-benzyl)-1H-indole-2,3-dione (3.05 g) was dissolved in 45 mL of tert-butanol and Boc-piperazine (2.04 g), Pd2(dba)3 (164 mg), dicyclohexyl-(2′,4′,6′-triisopropyl-biphenyl-2-yl)-phosphane (217 mg), and potassium carbonate (1.84 g) were added. The mixture was stirred at 120° C. for 4 hours and then cooled to room temperature. The mixture was partitioned between ethyl acetate and water, and the organic layer was separated, dried over sodium sulfate and concentrated under reduced pressure. The residue was purified by chromatography to afford 1.80 g of 4-[1-(3-fluoro-benzyl)-2,3-dioxo-2,3-dihydro-1H-indol-4-yl]-piperazine-1-carboxylic acid tert-butyl ester. MS: 340 (M−Boc+H)+.

Provenance & Evidence