1-Hydroxybenzotriazole → HCID 53328220, compound

Participants

Reaction Conditions

Reaction Steps

1-ethylpyrrole-2-carboxylic acid (139 mg, 1.0 mmol) was dissolved in DMF (3.0 ml), and WSCD (230 mg, 1.2 mmol), HOBt (168 mg, 1.2 mmol), and N-(1-(4-(2-morpholinoethylcarbamoyl)phenyl)-piperidin-4-yl)-1-piperazinecarboxamide (400 mg, 0.9 mmol) obtained in Example 15(5) was added thereto, followed by stirring under heat at 80° C. for 14 hours. After the reaction mixture was allowed to cool to room temperature, a saturated sodium bicarbonate aqueous solution was added to the reaction mixture, followed by extraction with chloroform. The extract was washed with water and saturated sodium chloride, and then dried over anhydrous sodium sulfate. After the desiccant was filtered off, the residue obtained by evaporation under reduced pressure was purified using medium-pressure silica gel flash column chromatography (methanol:chloroform=1:30 to 1:10), thereby obtaining 4-((1-ethylpyrrol-2-yl)-carbonyl)-N-(1-(4-(2-morpholinoethylcarbamoyl)phenyl)-piperidin-4-yl)-1-piperazinecarboxamide (213 mg, 42%) as a milky-white solid.

Provenance & Evidence