1,4-Dioxane → 1,1-dimethylethyl N-((5-fluoro-4-hydroxy-1,1-dimethyl-2-oxo-naphthalen-3-yl)carbonyl)glycinate

Participants

Reaction Steps

DIPEA (0.14 mL, 809 mmol, tert-butylglycine hydrochloride (136 mg, 809 μmol), and ethyl 5-fluoro-4-hydroxy-1,1-dimethyl-2-oxo-naphthalene-3-carboxylate (150 mg, 539 μmol) were heated to 75° C. in dioxane (4 mL) for 3 hours. The resulting mixture was cooled to room temperature and concentrated in vacuo. The residue was purified by flash chromatography to give 116 mg of 1,1-dimethylethyl N-((5-fluoro-4-hydroxy-1,1-dimethyl-2-oxo-naphthalen-3-yl)carbonyl)glycinate as a white solid. MS m/e=386 (M+Na)+.

Provenance & Evidence