Iron-Catalyzed C-H Alkynylation through Triazole Assistance: Expedient Access to Bioactive Heterocycles

Abstract

Triazole assistance enabled the first iron-catalyzed C-H alkynylation of arenes, heteroarenes, and alkenes. The modular TAM directing group set the stage for a sequential C-H alkynylation/annulation strategy with ample scope, enabling the iron-catalyzed assembly of isoquinolones, pyridones, pyrrolones, and isoindolinones with high levels of chemo-, site-, and regioselectivity.

Keywords: C−H activation; alkynes; heterocycles; iron; mechanism.