Triethylamine → HCID 45100906, compound

Participants

Reaction Steps

To a solution of 4-((S)-4-hydroxy-6-aza-spiro[2.5]oct-6-yl)-2-[3-methyl-2-oxo-4-(3-trifluoromethoxy-phenyl)-piperazin-1-yl]-butyric acid (example 48; 40 mg, 82 μmol) in N,N-dimethylformamide (1.5 mL) was added dimethylamine hydrochloride (10 mg, 0.12 mmol), triethylamine (33 mg, 0.33 mmol) and O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (38 mg, 99 μmol), then after 1 h the reaction mixture was partitioned between EtOAc and sat. aq. NaHCO3 solution. The organic layer was washed with brine, dried (MgSO4), filtered, and evaporated. Chromatography (IST Isolute® Flash NH2; EtOAc) afforded the title compound (30 mg, 71%). Colorless oil, MS: 513.5 (M+H)+.

Provenance & Evidence