Tandem vinyl radical Minisci-type annulation on pyridines: one-pot expeditious access to azaindenones

A new regiospecific alkylative/alkenylative cascade annulation of pyridines has been achieved whilst the corresponding classic Minisci alkylative annulation failed. This protocol provides a novel and expeditious access to azaindenones and related compounds via cross-dehydrogenative coupling with the long-standing problem of C2/C4 regioselectivity of pyridines being well addressed.

Automated summary

A new regiospecific alkylative/alkenylative cascade annulation of pyridines has been achieved, providing a novel approach to synthesizing azaindenones and related compounds. The long-standing issue of C2/C4 regioselectivity of pyridines has been effectively addressed in this protocol.