1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 2,6-difluoro-N-methoxy-N-methylnicotinamide

Participants

Reaction Steps

N,O-dimethylhydroxylamine hydrochloride (14.7 g), WSC (28.9 g), and HOBt (20.4 g) were added to a solution of 2,6-difluoronicotinic acid (6 g) and diisopropylethylamine (10 mL) in DMF (100 mL), and the reaction solution was stirred at room temperature for two days. Water and ethyl acetate were added to the reaction solution, and the organic layer was separated. The organic layer was dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The resulting residue was purified by silica gel column chromatography (carrier: Chromatorex NH; elution solvent: ethyl acetate) to obtain 7.01 g of the title compound.

Provenance & Evidence