Dimethylformamide → HCID 178501288, compound

Participants

Reaction Steps

In DMF (10 ml), EDC•HCl (274 mg, 1.43 mmol), DMAP (catalytic amount), and HOBt (catalytic amount) were added to (5-chloro-2-fluoro-4-((1-methyl-3-indolylcarbonyl)amino)phenyl)acetic acid (344 mg, 0.953 mmol) and methyl trans-4-((2S)-pyrrolidinylmethoxy)-1-cyclohexanecarboxylate (230 mg, 0.953 mmol) and the resulting mixture was stirred at room temperature for 15 hours. To the reaction mixture were added ethyl acetate (200 ml) and saturated brine (100 ml). The organic layer thus separated was washed with saturated brine (100 ml), dried over anhydrous magnesium sulfate, and distilled under reduced pressure to remove the solvent. From chloroform-ethyl acetate (4:1) eluate fractions, methyl trans-4-(1((5-chloro-2-fluoro-4-(1-methyl-3-indolylcarbonylamino)phenyl)acetyl)-(2S)-pyrrolidinylmethoxy)-1-cyclohexanecarboxylate (556 mg, 100%) was obtained as a pale yellow oil.

Provenance & Evidence