A novel and highly efficient dehydrogenative cross-coupling reaction between α-amino
carbonyl compounds and azoles by copper catalysis using di-tert-butyl peroxide (DTBP) as an oxidant is described. A diverse range of azoles undergo
the dehydrogenative imidoylation smoothly with various α-amino carbonyl compounds
for the exclusive formation of the corresponding N-imidoyl azoles in high yields under air. The synthetic method has the advantages
of good functional-group tolerance, wide substrate scope, excellent yields, and simple
operation, thus providing a convenient and practical protocol for the synthesis of
functionalized azoles.
Key words
copper - dehydrogenation - imidoylation - azoles - α-amino ketones