Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
7.4
4.2
Journals
Molecules
Special Issues
Cyclization Reactions in the Synthesis of Heterocyclic Compounds
molecules-logo
Submit to Special Issue Submit Abstract to Special Issue Review for Molecules Propose a Special Issue

Journal Menu

► Journal Menu

Journal Browser

► Journal Browser
share announcement

Cyclization Reactions in the Synthesis of Heterocyclic Compounds

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Organic Chemistry".

Deadline for manuscript submissions: 31 July 2025 | Viewed by 3466

Special Issue Editors

Dr. Yanping Zhu

E-Mail Website
Guest Editor
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Yantai University, Yantai 264005, China
Interests: heterocycles synthesis; oxidative cyclization; domino reactions; metal-catalysis; radical reactions
Prof. Dr. Anxin Wu

E-Mail Website
Guest Editor
National Key Laboratory of Green Pesticide, College of Chemistry, Central China Normal University, Wuhan 430079, China
Interests: heterocycles synthesis; natural products synthesis; domino reactions; synthetic tool-box based on the I2 /DMSO-mediated synthesis of (hetero)aromatic compounds

Special Issue Information

Dear Colleagues,

Heterocyclic compounds are widely present in various natural products, top-selling drugs, drug candidates, agrochemicals and materials. They play a significant role in most fields of sciences such as medicinal chemistry, biochemistry, agrochemistry, materials science and other areas of science. Among the top 200 small molecule drugs in the world sales rankings in 2022, there are 163 drugs with heterocyclic structures. Developing a highly efficient methodology for diverse heterocycle synthesis is still very desirable and urgent. This will resolve the issue of a large demand for compounds in drug discovery. Thus, it is necessary to develop new synthetic strategies to increase the diversity and complexity of heterocyclic molecules.

The expectation and goal of this Special Issue is to collect original research papers, mini-reviews, reviews and perspective articles devoted to all aspects of heterocyclic compounds, including cyclization reactions, annulation reactions, cycloaddition reactions, metal-catalyzed reactions, photo/electro-catalyzed reactions and domino/cascade reactions. Submission of manuscripts describing heterocyclic compound synthesis and biological evaluation, natural product synthesis, heterocycle synthesis and photophysical properties is also encouraged.

Dr. Yanping Zhu
Prof. Dr. Anxin Wu
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • heterocyclic compounds
  • cyclization reactions
  • cycloaddition reactions
  • synthetic methodology
  • diversity and complexity
  • natural product
  • photo/electro-catalyzed reactions

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • e-Book format: Special Issues with more than 10 articles can be published as dedicated e-books, ensuring wide and rapid dissemination.

Further information on MDPI's Special Issue policies can be found here.

Published Papers (4 papers)

Download All Papers
Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

Jump to: Review

16 pages, 1917 KiB  
Article
Eco-Friendly and Efficient Synthesis of 2-Hydroxy-3-Hydrazono-Chromones Through α,β-C(sp2)–H Bond Difunctionalization/Chromone Annulation Reaction of o-Hydroxyaryl Enaminones, Water, and Aryldiazonium Salts
by Xiaohong Wang, Menglin Peng, Yijin Wang, Siyu Song, Ying Xu, Li Chen and Fuchao Yu
Molecules 2025, 30(6), 1194; https://doi.org/10.3390/molecules30061194 - 7 Mar 2025
Viewed by 436
Abstract
A novel, eco-friendly, and efficient method for constructing 2,3-disubstituted chromone skeletons from readily available water, o-hydroxyaryl enaminones (o-HPEs), and aryldiazonium salts has been developed under mild reaction conditions. This α,β-C(sp2)–H bond difunctionalization/chromone annulation reaction strategy [...] Read more.
A novel, eco-friendly, and efficient method for constructing 2,3-disubstituted chromone skeletons from readily available water, o-hydroxyaryl enaminones (o-HPEs), and aryldiazonium salts has been developed under mild reaction conditions. This α,β-C(sp2)–H bond difunctionalization/chromone annulation reaction strategy is achieved by building two C(sp3)–O bonds and a C(sp2)-N bond, which provides a practical pathway for the preparation of 2-hydroxy-3-hydrazono-chromones in moderate to excellent yields, enabling broad substrate scope and good functional group tolerance, as well as gram-scale synthesis. This protocol offers a valuable tool for synthesizing diverse functionalized chromones with potential applications in drug discovery and industrial synthesis. Full article
(This article belongs to the Special Issue Cyclization Reactions in the Synthesis of Heterocyclic Compounds)
►▼ Show Figures

Graphical abstract

15 pages, 1926 KiB  
Article
Pyridoxal and Salicylaldehyde Derivatives: Synthesis, Characterization, and Antifungal Potential Against Opportunistic Yeast Pathogens
by Jairo Camacho, Carlos A. Bejarano, John E. Diaz, Yerly Vargas-Casanova, Silvia Katherine Carvajal, Valentina Diaz Santoyo, Claudia M. Parra-Giraldo and Alix E. Loaiza
Molecules 2025, 30(5), 1165; https://doi.org/10.3390/molecules30051165 - 5 Mar 2025
Viewed by 648
Abstract
This study reports the synthesis, characterization, and antifungal evaluation of a series of pyridoxal and salicylaldehyde derivatives, using synthetic methodologies such as radical cyclizations and click chemistry. Compounds 6a and 6b, featuring a fused dihydrobenzoxepine-pyridine scaffold, demonstrated effective fungicidal activity with MIC [...] Read more.
This study reports the synthesis, characterization, and antifungal evaluation of a series of pyridoxal and salicylaldehyde derivatives, using synthetic methodologies such as radical cyclizations and click chemistry. Compounds 6a and 6b, featuring a fused dihydrobenzoxepine-pyridine scaffold, demonstrated effective fungicidal activity with MIC values of 19 µg/mL against Cryptococcus neoformans 2807. Similarly, compound 6b exhibited notable activity with a MIC of 75 µg/mL against Candida auris PUJ-HUSI 537. Both compounds outperformed fluconazole (FLC) in these strains. In silico ADMET profiling revealed favorable pharmacokinetic properties, including blood–brain barrier penetration and drug-likeness parameters consistent with Lipinski’s rule of five. Cytotoxicity assays on human fibroblasts confirmed the low toxicity of compound 6a at the tested concentrations. These results highlight the potential of the fused dihydrobenzoxepine-pyridine scaffold as a promising antifungal candidate for further investigations. Full article
(This article belongs to the Special Issue Cyclization Reactions in the Synthesis of Heterocyclic Compounds)
►▼ Show Figures

Figure 1

20 pages, 5031 KiB  
Article
5-Aminopyrazole Dimerization: Cu-Promoted Switchable Synthesis of Pyrazole-Fused Pyridazines and Pyrazines via Direct Coupling of C-H/N-H, C-H/C-H, and N-H/N-H Bonds
by Yi-Xin Chai, Jun-Jie Ren, Yi-Ming Li, Yi-Cheng Bai, Qing-Qing Zhang, Yi-Zhen Zhao, Xue Yang, Xiao-Han Zhang, Xin-Shuang Zhang, An-Xin Wu, Yan-Ping Zhu and Yuan-Yuan Sun
Molecules 2025, 30(2), 381; https://doi.org/10.3390/molecules30020381 - 17 Jan 2025
Viewed by 646
Abstract
A Cu-promoted highly chemoselective dimerization of 5-aminopyrazoles to produce pyrazole-fused pyridazines and pyrazines is reported. The protocol generates switchable products via the direct coupling of C-H/N-H, C-H/C-H and N-H/N-H bonds, with the merits of broad substrate scope and high functional group compatibility. Gram-scale [...] Read more.
A Cu-promoted highly chemoselective dimerization of 5-aminopyrazoles to produce pyrazole-fused pyridazines and pyrazines is reported. The protocol generates switchable products via the direct coupling of C-H/N-H, C-H/C-H and N-H/N-H bonds, with the merits of broad substrate scope and high functional group compatibility. Gram-scale experiments demonstrated the potential applications of this reaction. Moreover, the preliminary fluorescence results uncovered that dipyrazole-fused pyridazines and pyrazines may have some potential applications in materials chemistry. Full article
(This article belongs to the Special Issue Cyclization Reactions in the Synthesis of Heterocyclic Compounds)
►▼ Show Figures

Figure 1

Review

Jump to: Research

18 pages, 6951 KiB  
Review
Glycine-Based [3+2] Cycloaddition for the Synthesis of Pyrrolidine-Containing Polycyclic Compounds
by Tieli Zhou, Xiaofeng Zhang, Desheng Zhan and Wei Zhang
Molecules 2024, 29(23), 5726; https://doi.org/10.3390/molecules29235726 - 4 Dec 2024
Cited by 1 | Viewed by 1030
Abstract
The synthesis of pyrrolidine compounds with biological interest is an active research topic. Glycine could be a versatile starting material for making pyrrolidine derivatives. This review covers recent works on glycine-based [3+2] cycloaddition and combines other annulation reactions in the one-pot synthesis of [...] Read more.
The synthesis of pyrrolidine compounds with biological interest is an active research topic. Glycine could be a versatile starting material for making pyrrolidine derivatives. This review covers recent works on glycine-based [3+2] cycloaddition and combines other annulation reactions in the one-pot synthesis of pyrrolidine-containing heterocyclic compounds. Synthetic method development, substrate scope, and reaction mechanisms are discussed. Applications of the compounds in drug discovery are briefly mentioned. This paper is helpful for chemists in the development of efficient and sustainable methods for the preparation of bioactive pyrrolidine compounds. Full article
(This article belongs to the Special Issue Cyclization Reactions in the Synthesis of Heterocyclic Compounds)
►▼ Show Figures

Graphical abstract

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-4
Back to TopTop