Hydrochloric Acid → HCID 86731314, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of methyl 4-fluoro-5-(methoxymethoxy)pyridine-2-carboxylate (1.80 g) in THF (20 mL) was added 6 N hydrochloric acid (5 mL), and the mixture was stirred at 70° C. for 20 min. To the reaction mixture was added saturated brine, and the mixture was extracted with ethyl acetate. The extract was dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was dissolved in DMF (20 mL), potassium carbonate (2.31 g) and (bromomethyl)cyclopropane (1.22 mL) were added thereto, and the mixture was stirred with heating at 70° C. for 1 hr. The reaction mixture was allowed to cool to room temperature, diluted with ethyl acetate, washed with saturated brine, and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ethyl acetate) to give the title compound (1.07 g).

Provenance & Evidence