Abstract

O-Methyl hydroxamic acids, readily available from carboxylic acids, are found to be extremely reactive for β-C−H activation by Pd(OAc)2. This reactivity is exploited to develop the first example of cross-coupling sp3 C−H bonds with sp3 boronic acids. Air was shown to be a suitable stoichiometric oxidant for the catalytic oxidative coupling reaction. A biologically active natural product is readily converted to its novel analogues through this coupling reaction.