A metal-free and triphosgene-free annulation of diamines with 4-chloro-3-nitrocoumarins enables efficient synthesis of polycyclic benzimidazoheterocycles via extrusion of nitromethane.
A novel cascade radical addition/cyclization reaction of non-activated olefins and oxamic acids has been proposed.
This review highlights halogen-mediated C2/C3 functionalization of indoles using molecular halogens and N-halosuccinimides for diverse bond-forming transformations, offering an efficient platform for sustainable indole functionalization.
A straightforward, moisture insensitive, and regioselective FeIII–CuII/p-TSA–CuI combocatalysed reaction is achieved from isatins and 2-alkynylanilines to diverse 12-benzoyl/benzyl/alkyl indolo[1,2-c]quinazolin-6(5H)-ones with gram-scale scalability and high atom economy.
This review will be an essential toolbox for medicinal and bioorganic chemists seeking novel multifunctional hybrid and bioactive N-heterocycles for drug discovery. The work highlights the need for and relevance of unexplored bioisosterism employing isoquinoline-based small-molecules in drug design.