Toolkit of reagents to aid drug discovery

Reagents have been developed that allow carbon—hydrogen bonds on benzene-like compounds called heterocycles to be converted directly into carbon—carbon bonds. The finding will be a boon to medicinal chemists. See Letter p.95 Functionalized heterocycle synthesis Nitrogen-rich heterocycles feature widely in pharmaceuticals, and their synthesis has been simplified by a series of advances in transition-metal-mediated cross-coupling reactions. However, the development of practical and selective C–H functionalization methods that do not rely upon pre-functionalized starting materials is an underdeveloped area. Here the authors report that zinc sulphinate salts can be used to transfer alkyl radicals to heterocycles, allowing for a mild, direct and operationally simple formation of medicinally relevant C–C bonds while reacting in an orthogonal fashion to other innate C–H functionalization methods.