Diisopropylethylamine → 3-((3S,4S)-3-fluoro-4-(3-fluoro-4-methoxyphenyl)piperidin-1-yl)-1-(3-fluoro-4-methylbenzyl)-pyrrolidin-2-one

Participants

Reaction Conditions

Reaction Steps

A mixture of (3S,4S)-3-fluoro-4-(3-fluoro-4-methoxyphenyl)piperidine hydrochloride (30 mg, 0.11 mmol, from step G), 3-bromo-1-(3-fluoro-4-methylbenzyl)pyrrolidin-2-one (54 mg, 0.19 mmol, intermediate 6,) and DIPEA (0.02 mL, 0.11 mmol) in DMF (3 mL) was heated to 120° C. for 90 min in a microwave reactor. The reaction mixture was cooled to rt and the solvent was removed under reduced pressure to obtain 60 mg of 3-((3S,4S)-3-fluoro-4-(3-fluoro-4-methoxyphenyl)piperidin-1-yl)-1-(3-fluoro-4-methylbenzyl)-pyrrolidin-2-one (diastereomeric pair), which was used in the next step without purification. LCMS (Method P) RT=1.12 min, m/z 433 (M+H+).

Provenance & Evidence