Potassium Carbonate → HCID 67510086, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of tert-butyl 1-(4-bromophenyl)-6-(methoxymethyl)-3-aza-bicyclo[3.1.0]hexane-3-carboxylate (Intermediate IX, 890 mg, 2.33 mmol) in 1,4-dioxane (15 mL), was added 2-pyrrolidinone (0.177 mL, 2.33 mmol), (±)-trans-1,2-diamine (0.139 mL, 1.16 mmol), CuI (221.3 mg, 1.16 mmol) and potassium carbonate (643 mg, 4.66 mmol) under nitrogen atmosphere. The reaction mixture was heated at 120° C. for 36 h. After completion of the reaction as confirmed by TLC, the solvent was removed in vacuo to afford the crude compound, which was purified by column chromatography (silica gel, 2:8 EtOAc:Pet. ether) to afford pure tert-butyl 6-(methoxymethyl)-1-(4-(2-oxopyrrolidin-1-yl)phenyl)-3-aza-bicyclo[3.1.0]hexane-3-carboxylate (600 mg, 66%) as a viscous oil.

Provenance & Evidence