Abstract
Comprehensive SummaryAxially chiral N‐arylindoles bearing a stereogenic C—N axis are unique important scaffolds in natural products, advance materials, pharmaceuticals and privileged chiral ligands or catalysts. Herein, we report the direct synthesis of C—N axially chiral N‐arylindoles through a Pd‐catalyzed free amine‐directed atroposelective C—H olefination enabled by a spiro phosphoric acid (SPA) ligand. A wide range of enantioenriched N‐aromatic amine indoles were obtained in high yields with good enantioselectivities (35 examples, up to 91% yield and up to 96% ee). The chiral products with free amine group offer an effective functional handle for down‐stream diversity‐oriented synthesis.
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