Sodium cyanoborohydride → HCID 86650668, compound

Participants

Reaction Steps

Dissolve (±)-3-[1-methyl-1-(6-trifluoromethyl-pyridin-2-yl)-ethylamino]-1-(4-difluoromethoxy-phenyl)-5-(2-fluoro-phenyl)-1,5-dihydro-pyrrol-2-one (2.06 g; 3.95 mmol) in HOAc (20 mL) and add sodium cyanoborohydride (0.50 g, 7.90 mmol). Stir for 2 hours at ambient temperature. Concentrate under reduced pressure and dissolve the residue in EtOAc. Wash the organic phase with 1N NaOH, water, saturated sodium chloride solution, dry over sodium sulfate, filter and concentrate under reduced pressure. Purify by silica gel chromatography (5-25% EtOAc-hexane) to yield (±)-3-[1-methyl-1-(6-trifluoromethyl-pyridin-2-yl)-ethylamino]-5-(2-fluoro-phenyl)-1-(4-difluoromethoxy-phenyl)-pyrrolidin-2-one (1.5 g, 73%), a racemic mixture, as a clear colorless oil. LC-MS ESI m/z: 524 (M+H)+, Tr=3.18 min., method 1.

Provenance & Evidence