1-Hydroxybenzotriazole → HCID 86683891, compound

Participants

Reaction Steps

A mixture of 2-(3,5-dimethoxyphenylamino)-5-fluoro-6-oxo-1,6-dihydropyridin-3-carboxylic acid (200 mg), WSC.HCl (312 mg), HOBt.H2O (249 mg), and DMF (2 ml) was stirred at room temperature for 45 minutes. 25% ammonia water (1 ml) was added, followed by stirring at the same temperature for 2 hours. Ethyl acetate was added to the reaction mixture. The resultant was washed with saturated saline and dried over anhydrous magnesium sulfate, the solvent was distilled away under reduced pressure. The obtained residue was purified by silica gel chromatography (hexane:ethyl acetate=7:3 to 1:1), and a yellow solid of 6-(1H-1,2,3-benzotriazol-1-yloxy)-2-(3,5-dimethoxyphenylamino)-5-fluoronicotinamide (109 mg) was thus obtained.

Provenance & Evidence