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Brønsted-acid-mediated dearomative cascade annulation of pyridines: one-pot synthesis of indolizin-5(3H)-one derivatives.

Created on 14 Sep 2026

Authors

Shashikant Tiwari, Nitin Kumar, Sukriti Santra, Diwan S Rawat

Published in

Chemical communications (Cambridge, England). Sep 14, 2026. Epub Sep 14, 2026.

Abstract

A direct dearomative cascade annulation of unactivated pyridines has been achieved using a Brønsted acid, enabling efficient access to indolizin-5(3H)-one frameworks. The transformation proceeds through a sequential [2+2] cycloaddition, followed by demethylation and intramolecular cyclization, furnishing fused bicyclic architectures in a one-pot two-step manner, using inexpensive hydrochloric acid. Deuterium incorporation studies further provide selectively deuterated indolizinone derivatives, offering opportunities for further synthetic diversification.

PMID:
42734040
Bibliographic data and abstract were imported from PubMed on 14 Sep 2026.

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