Photocatalytic Regioselective Alkylation of 4-Alkenylpyridines via Delocalized Pyridinyl Radicals

The control of selectivity in delocalized radical systems remains a formidable challenge in synthetic chemistry. We report a photocatalytic strategy for the regioselective alkylation of 4-alkenylpyridines using 4-alkyl-1,4-dihydropyridines (alkyl-DHPs) as radical precursors. The reaction proceeds via delocalized pyridinyl radicals, enabling radical-radical cross-coupling that delivers C6-alkylated products with exclusive regioselectivity, contrasting with the C4-selective pathway observed for simple pyridinyl radicals. Mechanistic studies and DFT calculations reveal that reversible formation of an unstable C4-coupled intermediate funnels the reaction toward the thermodynamically favored C6 pathway.

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Publication Details

Journal
Organic Letters
Published
2026-05-09
DOI
https://doi.org/10.1021/acs.orglett.6c01471
Primary Topic
Radical Photochemical Reactions
Type
article
Field-Weighted Citation Impact
0.00

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article

Photocatalytic Regioselective Alkylation of 4-Alkenylpyridines via Delocalized Pyridinyl Radicals

Zehua Zhou, Kemeng Du, Zhichao Zhang, Pan Xu
Organic Letters
Radical Photochemical Reactions
article

Photocatalytic Regioselective Alkylation of 4-Alkenylpyridines via Delocalized Pyridinyl Radicals

Zehua Zhou, Kemeng Du, Zhichao Zhang, Pan Xu
article en

Abstract

The control of selectivity in delocalized radical systems remains a formidable challenge in synthetic chemistry. We report a photocatalytic strategy for the regioselective alkylation of 4-alkenylpyridines using 4-alkyl-1,4-dihydropyridines (alkyl-DHPs) as radical precursors. The reaction proceeds via delocalized pyridinyl radicals, enabling radical-radical cross-coupling that delivers C6-alkylated products with exclusive regioselectivity, contrasting with the C4-selective pathway observed for simple pyridinyl radicals. Mechanistic studies and DFT calculations reveal that reversible formation of an unstable C4-coupled intermediate funnels the reaction toward the thermodynamically favored C6 pathway.

Organic Letters
National Natural Science Foundation of China, Natural Science Foundation of Jiangsu Province, Southeast University
Clean water and sanitation
Openalex Percentile: Top 9%
Radical Photochemical Reactions
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