Axially chiral indoline‐based scaffolds are virtually universal in biological and pharmaceutical compounds. In this study, we demonstrate the Rh‐catalyzed asymmetric [2 + 2 + 2] cycloaddition of 1,6‐enynes with steric hindered N‐alkynyl indoles, which… Click to show full abstract
Axially chiral indoline‐based scaffolds are virtually universal in biological and pharmaceutical compounds. In this study, we demonstrate the Rh‐catalyzed asymmetric [2 + 2 + 2] cycloaddition of 1,6‐enynes with steric hindered N‐alkynyl indoles, which enables simultaneous construction of both axial and central chirality, containing a quaternary carbon center, in one step. Notable features of these reactions include excellent chemo‐, regio‐, diastereo‐ and enantioselectivity, 100% atom‐economy, easily available SEGPHOS ligand, and mild conditions.
Journal Title: ChemCatChem
Year Published: 2024
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