反应详情

Heat a mixture of 5-(3-fluorophenylethynyl)-pyridine-3-carbaldehyde, (prepared essentially as described in EXAMPLE 89), (90 mg, 0.38 mmol) and methoxylamine hydrochloride (160 mg, 3.02 mmol) and potassium carbonate (260 mg, 1.89 mmol) in ethanol at 80° C. overnight. Cool to room temperature, filter solids and concentrate. Purify the residue by silica gel chromatography, eluting with 5:45:45 ethyl acetate:chloroform:hexanes, to give the title compound as a white solid (45 mg, 47%).

1. temperatureHeat
2. custom(prepared essentially
3. customat 80° C.
4. customovernight
5. filtrationfilter solids
6. concentrationconcentrate
7. customPurify the residue by silica gel chromatography
8. washeluting with 5:45:45 ethyl acetate