A novel
strategy for the synthesis of imidazo-fused polycyclic
compounds under mild, base-free, and silver-free conditions by a rhodium(III)-catalyzed
C–H annulation of alkenyl or arylimidazoles and (hetero)cyclic
1,3-dicarbonyl compounds is reported here. Such a step-economic protocol
features the selective cleavage of two different C–H bonds
in one step, featuring easy operation, readily available starting
materials, gram-scale synthesis, broad functional group tolerance,
and no requirement to presynthesize carbene precursors. Notably, the
synthetic potential is showcased by the structural modification of
drug and the highly step-economic synthesis of Janus kinase inhibitor
in only three steps with a satisfactory 26% total yield (previous
method: in nine steps with 0.6% yield).
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.