Water → HCID 19434881, compound

Participants

Reaction Steps

438 mg (0.984 mmol) of the above 2-[4-(3-azidopropylamino)-3-fluorophenyl]-5-butylamino-6,8-difluoro-4H-1-benzopyran-4-one was dissolved in 25 mL of tetrahydrofuran, 389 mg (1.48mmol) of triphenylphosphine was added under ice-cooling and the mixture was stirred at room temperature for 1 hour. 25 mL of water was added thereto and the mixture was further stirred for 5.5 hours. The mixture was extracted twice with ethyl acetate, and the organic layer was washed once with an aqueous saturated solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure and the residue was purified by silica gel column chromatography (chloroform:methanol:aqueous ammonia=9:1:1) to give 380 mg of Compound 126 (yield: 92%), which was converted to hydrochloride according to the conventional method.

Provenance & Evidence