Dimethylformamide → HCID 66725920, compound

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Reaction Steps

A mixture of 5-[4-(methylsulfonyl)phenoxy]-7-(tetrahydro-2H-pyran-4-yloxy)-1H-indole-2-carboxylic acid (1.95 g), 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (1.73 g), 1-hydroxybenzotriazole ammonium salt (1.37 g), and N,N-dimethylformamide (50 mL) was stirred at room temperature for 12 hr. Water was added to the reaction solution, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over magnesium sulfate, filtered and concentrated under reduced pressure. The obtained crude product was subjected to silica gel column chromatography (methanol:ethyl acetate:hexane=0:85:15 to 10:90:0, volume ratio) to give the title compound (2.06 g, yield 100%) as a white solid.

Provenance & Evidence