Potassium Carbonate → HCID 67340992, compound

Participants

Reaction Steps

A mixture of 7-amino-5-bromo-4-(4-fluorophenyl)-2,2-dimethyl-2H-1,4-benzoxazin-3(4H)-one (compound obtained in Reference Example 53(7); 140 mg), potassium carbonate (159 mg), dioxane (11 mL), trimethylboroxin (134 μL) and [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II) (31 mg) was refluxed under argon atmosphere for 2 hours. After cooling, to the reaction mixture was added water, and the mixture was extracted with ethyl acetate. The organic layer was washed with brine, dried over magnesium sulfate and concentrated in vacuo. The resultant residue was purified by column chromatography on silica gel (solvent; n-hexane/ethyl acetate=3/1→3/7) to give 7-amino-4-(4-fluorophenyl)-2,2,5-trimethyl-2H-1,4-benzoxazin -3(4H)-one (102 mg) as a pale yellow powder.

Provenance & Evidence