Iodoethane → 3-(2,3-Difluorophenyl)-1-ethylpyrrolidin-3-ol

Participants

Reaction Steps

Preparation according to Example 2: 3-(2,3-difluorophenyl)pyrrolidin-3-ol (0.30 g, 1.50 mmol), acetonitrile (3 mL), potassium carbonate (0.21 g, 1.50 mmol), iodoethane (0.12 mL, 1.50 mmol). Microwave irradiation at 100° C. for 20 minutes. Purification by HPLC on Waters OBD C18, 5 μm (MeOH/33 mM NH3, 1:1). The amine was converted to the fumaric acid salt and recrystallized from ethanol/diethyl ether/diisopropyl ether: M.p. 119-120° C.; MS m/z (relative intensity, 70 eV) 227 (M+, 14), 212 (11), 141 (14), 127 (11), 71 (bp).

Provenance & Evidence