Tetrahydrofuran → trans-(+/-)-4-(4-Chloro-3-fluorophenoxy)-1-methylpyrrolidin-3-amine

Participants

Reaction Steps

To a solution of 426 (0.480 g, 1.77 mmol), PPh3 (0.930 g, 3.54 mmol) and THF (10 mL) was added H2O (1.0 mL). The resultant mixture was heated at 55° C. for 3 h. The solvent was removed in vacuo. The residue was purified by SiO2 chromatography eluting with DCM/MeOH (5:1 DCM/MeOH then 1:1) to afford 85 mg (21% over 5 steps) of trans-(±)-4-(4-chloro-3-fluorophenoxy)-1-methylpyrrolidin-3-amine (428): LC-MS (ESI) m/z 245 (M+H).

Provenance & Evidence