Triethylamine → 3-{6-Chloro-2-fluoro-3-[4-(4-methyl-piperazin-1-yl)-4-oxo-butyl]-benzyl}-1-cyclohexyl-pyrrolidin-2-one

Participants

Reaction Conditions

Reaction Steps

Add 4-[4-chloro-3-(1-cyclohexyl-2-oxo-pyrrolidin-3-ylmethyl)-2-fluoro-phenyl]-butyric acid (Preparation 80) (200 mg, 0.22 mmol), EDAC (63 mg, 0.33 mmol), HOBT (45, mg, 0.33 mmol), triethylamine (0.1 mL, 0.7 mmol) and 1-methylpiperazine (0.1 mL, 0.9 mmol) in THF (5 mL). Heat the mixture at 80° C. for 3 hours. Evaporate solvent and purify the residue by column chromatography to give the title product as white solid: Mass spectrum (ion spray): m/z=478.3 (M+H).

Provenance & Evidence