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

Participants

Reaction Steps

To a stirred solution of (S)-tetrahydro-furan-2-carboxylic acid (described in J. Med. Chem., 1995, 38(15, 2830) (5.0 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 5.1 mg (25%) of the title compound.

Provenance & Evidence