反应详情

To a solution of 5-[(2,5-difluorophenyl)[(4-fluorophenyl)sulfonyl]methyl]-4-methylpyridine-2-carboxylic acid (222 mg, 0.527 mmol) obtained in Example 12 in methylene chloride (5 ml), 3-methylthiopropylamine (66 mg, 0.632 mmol), 1-hydroxybenzotriazole (71 mg, 0.527 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (121 mg, 0.632 mmol) and 4-methylmorpholine (69 μl, 0.632 mmol) were added. The reaction solution was stirred for 3 days at room temperature, and was concentrated under reduced pressure. The concentration residue was subjected to silica gel column chromatography, and the fraction obtained from an elution with ethyl acetate:methylene chloride (=1:20) was concentrated under reduced pressure, to obtain the title compound (253 mg, 0.497 mmol, 94%) as a white solid.

1. concentrationwas concentrated under reduced pressure
2. customthe fraction obtained from an elution with ethyl acetate
3. concentrationmethylene chloride (=1:20) was concentrated under reduced pressure