Post by Synthesis & Catalysis

🔄 Ring-Flipping to Success: Conformation-Controlled C3–H Arylation! ✅ This breakthrough paper introduces the first directed palladium-catalyzed site-selective C3-C(sp3)–H arylation of saturated azacycles by temporarily converting the native endocyclic nitrogen into a torsionally flexible N-oxide directing group, enabling a favorable five-membered cyclopalladation that was previously out of reach. ✅ This method unlocks a substituent-agnostic strategy to access highly valuable, complex 3-substituted saturated heterocycles with exceptional cis- or trans-diastereoselectivity, providing medicinal chemists with a robust tool to explore uncharted chemical space in drug discovery. 📅 Publication Date: June 02, 2026 🔗 Paper Link: https://lnkd.in/epvxNbjA ✍️ Authors: Chia-Yu Chen, Zhoulong Fan, Daniel A. Strassfeld, Hau Sun Sam Chan, Miguel Cohen Suarez, Md Emdadul Hoque, and Jin-Quan Yu #OrganicChemistry #Catalysis #CHActivation #SaturatedAzacycles #MedicinalChemistry #DrugDiscovery #PdCatalysis