Triethylamine → HCID 131727777, compound

Participants

Reaction Steps

Combine 4-methyl-pentanoic acid (0.047 mL, 0.37 mmol), 2-(R)-[(2-(R)-amino-1-(S)-hydroxy-3-(3,5-difluoro-phenyl)propyl)]piperzine-1-carboxylic acid tert-butyl ester (63 mg, 0.17 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (78 mg, 0.41 mmol), hydroxybenzotriazole (50 mg, 0.41 mmol), triethylamine (0.095 mL, 0.68 mmol), and 4-dimethylaminopyridine (4.6 mg, 0.04 mmol) in 2 mL dichloromethane. Stir at room temperature over night. Subject reaction mixture to silica gel chromatography, eluting with 97:3 dichloromethane:methanol. Stir residue in 4M HCl in 1,4-dioxane over night. Concentrate under reduced pressure to provide the title compound (39 mg, 49%) as a white solid.

Provenance & Evidence