Water → HCID 19435012, compound

Participants

Reaction Conditions

Reaction Steps

580 mg (1.05 mmol) of 7-bromo-6,8-difluoro-2-(3-fluoro-4-pivaloylaminophenyl)-5-pivaloylamino-4H-1-benzopyran-4-one obtained in Example 84 (2) was dissolved in 6 mL of dimethyl sulfoxide, 1.2 mL (10.5 mmol) of N-methylpiperazine was added and the mixture was stirred at 100° C. for 7 hours. Water was added to the reaction solution and the mixture was extracted twice with ethyl acetate. The organic layer was washed once with water and 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=20:1) to give 350 mg of 6,8-difluoro-2-(3-fluoro-4-pivaloylaminophenyl)-7-(4-methylpiperazin-1-yl)-5-pivaloylamino-4H-1-benzopyran-4-one (yield: 58%).

Provenance & Evidence