反应详情

温度

45 °C

Diisopropylethylamine (0.39 mL, 2.25 mmol) and 3,4,5-trifluoronitrobenzene (0.143 g, 0.81 mmol) were added to a solution 3-aza-bicyclo[3.1.0]hexane (prepared by the general procedure of Brighty, K. E., Castaldi, M. J. Synlett, 1996, 1097-1099; 0.106 g of the HCl salt, 0.9 mmol) in DMF (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-(2,6-difluoro-4-nitro-phenyl)-3-aza-bicyclo[3.1.0]hexane as a yellow solid.

1. customprepared by the general procedure of Brighty, K
2. temperaturecooled to room temperature
3. washwashed with 0.5 M HCl, saturated NaHCO3, brine
4. dry with materialdried (MgSO4)
5. filtrationThe mixture was filtered
6. concentrationconcentrated