Triethylamine → 2-(3,5-Bis-trifluoromethyl-phenyl)-n-[(3s,4r)-1-(4-methoxymethyl-cyclohexanecarbonyl)-4-phenyl-pyrrolidin-3-yl]-n-methyl-isobutyramide

Participants

Reaction Steps

To a stirred solution of 4-methoxymethyl-cyclohexanecarboxylic acid (described in JP60258141) (7.4 mg, 0.043 mmol) in THF (2 ml) at RT were added Et3N (12 μl, 0.086 mmol), BOP (25 mg, 0.057 mmol) and rac-2-(3,5-bis-trifluoromethyl-phenyl)-N-methyl-N-((3S,4R)-4-phenyl-pyrrolidin-3-yl)-isobutyramide (Intermediate VII-1) (20 mg, 0.043 mmol). Stirring was continued at 40° C. for 48 hours. Concentration and purification by preparative HPLC afforded 12.7 mg (48%) of the title compound.

Provenance & Evidence