Hydrochloric Acid → 3-aminomethyl-7-fluoro-1-(2-fluoro-phenyl)-1H-quinolin-4-one hydrochloride salt

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Reaction Steps

In a 50 mL round bottom flask, 3-azidomethyl-7-fluoro-1-(2-fluoro-phenyl)-1H-quinolin-4-one (0.290 g, 0.929 mmol) was added platinum (IV) oxide (0.040 g, 0.176 mmol) and 4 N HCl (2 mL) in 1:1 dichloroethane-ethyl acetate (15 mL). The reaction was charged with 1 atm. H2 using a balloon and stirred at room temperature for 3 hr. The catalyst was filtered off and the filtrate evaporated to dryness to give 3-aminomethyl-7-fluoro-1-(2-fluoro-phenyl)-1H-quinolin-4-one hydrochloride salt (200 mg, 67% yield). The crude was used in subsequent steps without further purification.

Provenance & Evidence