Pyridinium-Fused 1,3-Selenazoles via Cyclizations of 2-Pyridylselenyl Chloride with Alkynes: Synthesis, Structures, and Antifungal Properties

We report a straightforward and versatile synthetic route to pyridinium-fused 1,3-selenazoles via the electrophilic cyclization of 2-pyridylselenyl chloride with alkynes. The reaction proceeds efficiently under mild conditions with representative terminal and internal alkynes. While the cyclization exhibits high regioselectivity favoring the 3-substituted isomer for most substrates, reactions with 2-pyridyl- and 2-quinolylacetylenes yield regioisomeric mixtures. DFT calculations rationalize this divergence, revealing a competition between kinetic and thermodynamic control; the 3-isomer is kinetically favored, while the 2-isomer is thermodynamically stabilized by an ancillary chalcogen bond between the selenium atom and the pyridine nitrogen of the alkyne substituent. Molecular structures were confirmed by single-crystal X-ray diffraction, and the non-covalent interactions governing supramolecular assembly in the solid state were rigorously analyzed using MEP surfaces, the QTAIM, and NBO analysis. Antifungal evaluation identified several compounds with notable activity against phytopathogenic fungi, highlighting the potential of this novel heterocyclic scaffold in agrochemical applications.

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Publication Details

Journal
International Journal of Molecular Sciences
Published
2026-03-23
DOI
https://doi.org/10.3390/ijms27062908
Primary Topic
Organoselenium and organotellurium chemistry
Type
article
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article

Pyridinium-Fused 1,3-Selenazoles via Cyclizations of 2-Pyridylselenyl Chloride with Alkynes: Synthesis, Structures, and Antifungal Properties

Alexander G. Tskhovrebov, Evgeny A. Dukhnovsky, Olga Chusova, Francis Verpoort et al.
International Journal of Molecular Sciences
Organoselenium and organotellurium chemistry
article

Pyridinium-Fused 1,3-Selenazoles via Cyclizations of 2-Pyridylselenyl Chloride with Alkynes: Synthesis, Structures, and Antifungal Properties

Alexander G. Tskhovrebov, Evgeny A. Dukhnovsky, Olga Chusova, Francis Verpoort, R. Rodríguez Gomila, A.V. Borisov, Alexey S. Kubasov, Victor N. Khrustalev, Antonio Frontera, Zhishen Ge
article en

Abstract

We report a straightforward and versatile synthetic route to pyridinium-fused 1,3-selenazoles via the electrophilic cyclization of 2-pyridylselenyl chloride with alkynes. The reaction proceeds efficiently under mild conditions with representative terminal and internal alkynes. While the cyclization exhibits high regioselectivity favoring the 3-substituted isomer for most substrates, reactions with 2-pyridyl- and 2-quinolylacetylenes yield regioisomeric mixtures. DFT calculations rationalize this divergence, revealing a competition between kinetic and thermodynamic control; the 3-isomer is kinetically favored, while the 2-isomer is thermodynamically stabilized by an ancillary chalcogen bond between the selenium atom and the pyridine nitrogen of the alkyne substituent. Molecular structures were confirmed by single-crystal X-ray diffraction, and the non-covalent interactions governing supramolecular assembly in the solid state were rigorously analyzed using MEP surfaces, the QTAIM, and NBO analysis. Antifungal evaluation identified several compounds with notable activity against phytopathogenic fungi, highlighting the potential of this novel heterocyclic scaffold in agrochemical applications.

International Journal of Molecular SciencesVol. 27(6)
Peoples' Friendship University of Russia (RU), Wuhan University of Technology (CN), A. N. Nesmeyanov Institute of Organoelement Compounds (RU), N.D. Zelinsky Institute of Organic Chemistry (RU), NS Kurnakova Institute of General and Inorganic Chemistry (RU), Nizhny Novgorod State Pedagogical University (RU), Universitat de les Illes Balears (ES), Xi'an Jiaotong University (CN)
Openalex Percentile: Top 11%
Organoselenium and organotellurium chemistry
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