4-Methylmorpholine → HCID 57736436, compound

Participants

Reaction Steps

To a solution of 5-[(2,5-difluorophenyl) [(4-fluorophenyl)sulfonyl]methyl]-4-methylpyridine-2-carboxylic acid (99 mg, 0.235 mmol) obtained in Example 12 in methylene chloride (3 ml), N, O-dimethylhydroxyamine hydrochloride (28 mg, 0.282 mmol), 1-hydroxybenzotriazole (32 mg, 0.235 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride mg, 0.382 mmol) and 4-methylmorpholine (61 μl, 0.564 mmol) were added. The reaction solution was stirred for 5 days at room temperature, and was concentrated under reduced pressure. The resulting concentration residue was subjected to silica gel column chromatography, and the fraction obtained from an elution with hexane:ethylacetate (=1:1) was concentrated under reduced pressure. Ethyl acetate-hexane was added to the resulting concentration residue, and the solid thus precipitated was collected by filtration, to obtain the title compound (73 mg, 0.157 mmol, 67%) as a white powder.

Provenance & Evidence