Hydrochloric Acid → 3-(2-Fluoro-4-nitro-phenyl)-3-aza-bicyclo[3.1.0]hexane

Participants

Reaction Conditions

Reaction Steps

Diisopropylethylamine (0.56 mL, 3.2 mmol) and 3,4-difluoronitrobenzene (0.184 g, 1.16 mmol) were added to a solution 3-aza-bicyclo[3.1.0]hexane (0.152 g of HCl salt, 1.28 mmol; prepared as described in U.S. Pat. No. 4,183,857) in DMF (3.2 mL). The mixture was heated for three days at 45° C. and then cooled to room temperature. The solution was diluted with ethyl acetate and washed with 0.5 M HCl, saturated NaHCO3, brine, and dried (MgSO4). The mixture was filtered and concentrated to give 3-(2-fluoro-4-nitro-phenyl)-3-aza-bicyclo[3.1.0]hexane as a yellow solid.

Provenance & Evidence