An efficient and straightforward
synthesis of polysubstituted oxazol-2(3H)-ones has
been developed via a tandem Hofmann-type rearrangement
and cyclization reaction of various α-acyl-β-aminoacrylamides
mediated by phenyl iodine(III) bis(trifluoroacetate) (PIFA) in the
presence of trifloroacetic acid (TFA). This novel protocol features
readily available starting materials, mild reaction conditions, simple
execution, high chemoselectivity, good functional group tolerance,
and a metal-free oxidation process.