Triethylamine → HCID 66792790, compound

Participants

Reaction Steps

A mixture of 1-(2-tert-butyl-4-chlorophenyl)piperazine dihydrochloride (Reference Example 20, 0.50 g, 1.54 mmol), 5-hydroxypyridine-2-carboxylic acid (0.26 g, 1.84 mmol), triethylamine (644 μL, 4.62 mmol), EDCI (0.29 g, 1.84 mmol) and HOBt (0.28 g, 1.84 mmol) in N,N-dimethylformamide (10 mL) was stirred at room temperature for 5 days. The reaction mixture was added to saturated NaHCO3 solution and extracted with ethyl acetate. The extract was washed with saturated NaHCO3 solution, brine, dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ethyl acetate 50:50 to 0:100) to give the title compound (0.30 g, 52%) as a white powder.

Provenance & Evidence