Ethanolamine → HCID 57736426, compound

Participants

Reaction Steps

5-[(2,5-Difluorophenyl)[(4-fluoro-3-methylphenyl)sulfonyl]methyl]-4-methylpyridine-2-carboxylic acid (300 mg, 0.69 mmol), 2-aminoethanol (60 μl, 1.0 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (193 mg, 1.0 mmol), 1-hydroxybenzotriazole (93 mg, 0.69 mmol), and triethylamine (292 μl, 2.1 mmol) were dissolved in methylene chloride (60 ml), and the solution was stirred overnight at room temperature. Water was added to the reaction mixture, and the mixture was extracted twice with methylene chloride. The combined organic layer was dried over anhydrous sodium sulfate and filtered, and then the filtrate was concentrated under reduced pressure. The resulting residue was purified by preparative thin-layer chromatography (developed with 5% methanol/methylene chloride, eluted with 30% methanol/methylene chloride), to obtain the title compound (190 mg, 0.39 mmol, 58%) as a white amorphous substance.

Provenance & Evidence