4-Fluoro-N-methyl-benzenepropanamine → (2S,3R)-3-(dibenzylamino)-1-[[3-(4-fluorophenyl)propyl](methyl)amino]butan-2-ol

Participants

Reaction Steps

The product of Step e (1.30 g, 7.80 mmol, 1 eq.), (1R)-N,N-dibenzyl-1-[(2S)-oxiran-2-yl]ethanamine (the synthesis of which is described in Example 100) (2.08 g, 7.80 mmol, 1 eq.) and ethanol (10 mL) were mixed at 25° C. under N2 then refluxed overnight. Worked up by stripping off the ethanol then purifying the residue over silica gel in 1:1 Hexanes/EtOAc to 100% EtOAc. Obtained 1.16 g of an amber oil. MS (ESI) detects (M+H)+=435.

Provenance & Evidence