The regioselective Wacker oxidation of internal allylamines: synthesis of functionalized and challenging β-amino ketones

A convenient and general protocol for the palladium-catalysed oxidation of internal allylamine derivatives to β-amino ketones is reported. The transformation occurs at room temperature and shows a wide substrate scope as well as high functional group and N -protecting group tolerance. We also describe potential applications of the method, e.g. , the synthesis of bioactive molecules or simple transformations of selected β-amino ketones into other interesting building blocks. A general protocol for the Pd-catalysed oxidation of internal allylamine derivatives to β-amino ketones is reported. The transformation occurs at mild conditions and shows a wide substrate scope as well as high functional group tolerance.