Acetamide → HCID 57863417, compound

Participants

Reaction Steps

To Compound 10 (571 mg, 1 mmol) and acetic acid amide (89 mg, 1.5 mmol) was added and solved dioxane (12 ml), and were added cesium carbonate (48.8 mg, 1.5 mmol) and 4,5-bis(diphenylphosphino)-9,9-dimethylxancene (88 mg, 0.152 mmol), and palladium acetate (24 mg, 0.107 mmol) under stirring at room temperature in nitrogen gas flow, and then the solution was stirred for 5 hours under heating in an oil bath at 70° C. The mixture was added with ethyl acetate, water and ammonium chloride aqueous solution for extraction, washed with sodium chloride aqueous solution, dried over sodium sulfate and the subjected to distillation. The obtained residue was subjected to silica gel chromatography and recrystallized from acetone-diisopropyl ether, to give 5-acetylamino-8-benzyloxy-3-(4-fluorobenzyl)[1,6]naphthyridine-7-carboxylic acid (2-methoxyethyl) amide 12 (245 mg, 80.9%) as colorless crystals.

Provenance & Evidence