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.
- Practical and innate carbon–hydrogen functionalization of heterocycles (Letter p95, doi: 10.1038/nature11680)
Organic chemistryToolkit of reagents to aid drug discovery (News & Views p45, doi: 10.1038/nature11760)
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