Synthesis of Unprotected β‐Arylethylamines by Iron(II)‐Catalyzed 1,2‐Aminoarylation of Alkenes in Hexafluoroisopropanol
Résumé
Abstract β‐Arylethylamines are prevalent structural motifs in molecules exhibiting biological activity. Here we report a sequential one‐pot protocol for the 1,2‐aminoarylation of alkenes with hydroxylammonium triflate salts and (hetero)arenes. Unlike existing methods, this reaction provides a direct entry to unprotected β‐arylethylamines with remarkable functional group tolerance, allowing key drug‐oriented functional groups to be installed in a two‐step process. The use of hexafluoroisopropanol as a solvent in combination with an iron(II) catalyst proved essential to reaching high‐value nitrogen‐containing molecules.
Domaines
ChimieOrigine | Fichiers produits par l'(les) auteur(s) |
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