反应详情

Preparation according to Example 51. Enantiomer E1 of 3-(2,3-difluorophenyl)-pyrrolidin-3-ol (0.11 g, 0.55 mmol), acetonitrile (6 mL), potassium carbonate (0.140 g, 1 mmol) cyclopropylmethyl bromide (0.05 mL, 0.51 mmol). Flash chromatography on silica gel (Ethyl acetate/methanol, 10:1). Yield: 0.045 g. [α]D=+12.5°; The amine was converted to the oxalic acid salt and recrystallized from ethanol/diethyl ether/diisopropyl ether; Mp. 170-171° C.; MS m/z (relative intensity, 70 eV) 253 (M+, 27), 96 (bp), 97 (60), 55 (44), 141 (32), 98 (2).

1. customPreparation
2. customrecrystallized from ethanol/diethyl ether/diisopropyl ether