Chloroacetic Acid → HCID 10740435, compound

Participants

Reaction Conditions

Reaction Steps

100 g (1.06 mol) of chloroacetic acid and 30 mL of sulfuric acid were added to 10.8 g (20.0 mmol) of 6,8-difluoro-2-(3-fluoro-4-pivaloylaminophenyl)-7-hydroxymethyl-5-pivaloylamino-4H-1-benzopyran-4-one obtained in EXAMPLE 118 (4), and the mixture was stirred at 100° C. for 20 minutes. The reaction solution was poured into 1 L of ice-water and the mixture was extracted with ethyl acetate. The organic layer was washed with an aqueous saturated solution of sodium chloride and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was triturated with diisopropyl ether, to give 8.00 g of Compound 159 (yield: 97%).

Provenance & Evidence