An
efficient copper-catalyzed aerobic oxidative cross-dehydrogenative
coupling reaction for the synthesis of multisubstituted phosphorylhydrazides
from N,N-disubstituted hydrazines
and hydrogen phosphoryl compounds is accomplished. The reaction proceeds
under mild conditions without the addition of any external oxidants
and bases. This work reported here represents a direct P(O)–N–N
bond formation with the advantages of being operationally simple,
good functional group tolerance, and high atom and step economy. Furthermore,
the selected compounds exhibit potential inhibitory activity against
tumor cells, which can be used in the field of screening of anticancer
agents as new chemical entities.