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Advances in Organic Synthetic Chemistry

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Chemical and Molecular Sciences".

Deadline for manuscript submissions: 20 August 2025 | Viewed by 6308

Special Issue Editor


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Guest Editor
CIQSO—Center for Research in Sustainable Chemistry, Department of Chemistry, University of Huelva, 21071 Huelva, Spain
Interests: organic synthesis; supramolecular chemistry; host–guest chemistry; dyes; photochromics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

I am pleased to invite you to submit to this Special Issue in Applied Sciences, entitled “Advances in Organic Synthetic Chemistry”. We are seeking the latest research on advances and developments in novel methodologies in (bio)functional compound syntheses.

Studies of new reactions or synthetic methodologies are welcome. Manuscripts that focus on novel synthesized compounds for different applications, such as materials, photonics, biology, or electronics, among others, are also encouraged. We also seek submissions that develop protocols or processes that are more sustainable, atom-efficient, and without waste/residues, or that use greener solvents.

Original work highlighting the latest research developments is encouraged; however, review papers and perspective manuscripts are also welcome.

Dr. José A. González-Delgado
Guest Editor

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. Applied Sciences 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 2400 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

  • advanced organic synthesis
  • new synthetic methodologies
  • sustainable processes
  • (bio)functional compounds
  • green synthetic chemistry

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Published Papers (7 papers)

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Research

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11 pages, 490 KiB  
Article
Environmentally Friendly Green O-Alkylation Reaction for Ethenzamide Synthesis
by Paulina Niedziejko-Ćwiertnia, Anna Karolina Drabczyk, Damian Kułaga, Patrycja Podobińska, Wojciech Bachowski, Kamila Zeńczak-Tomera, Piotr Michorczyk, Ruilong Sheng and Jolanta Jaśkowska
Appl. Sci. 2025, 15(3), 1342; https://doi.org/10.3390/app15031342 - 27 Jan 2025
Viewed by 449
Abstract
Ethenzamide (2-ethoxybenzamide), besides acetylsalicylic acid, is one of the mostly used salicylic acid derivatives in pharmaceuticals. It has analgesic and anti-inflammatory effects that originate from the inhibition of cyclooxygenase (COX-1) activity, thus blocking prostaglandin synthesis. In this work, efficient and eco-friendly methods were [...] Read more.
Ethenzamide (2-ethoxybenzamide), besides acetylsalicylic acid, is one of the mostly used salicylic acid derivatives in pharmaceuticals. It has analgesic and anti-inflammatory effects that originate from the inhibition of cyclooxygenase (COX-1) activity, thus blocking prostaglandin synthesis. In this work, efficient and eco-friendly methods were developed for the synthesis of ethenzamide via the O-alkylation reaction of salicylamide. The reactions were carried out under conventional conditions in a solvent-free system using variant solvents and different phase transfer catalysts (PTC) in the presence of microwave radiation or ultrasonic conditions. It was shown that in solvent-free conditions using TBAB as a catalyst, ethenzamide can be obtained within 15 min at 80 °C with 79% yield. Meanwhile, using microwave radiation under the same conditions, the reaction time can be shortened to 90 s with 92% yield. Notably, high yields can be achieved under PTC in water (or organic solvent-free) conditions using microwave radiation (2 min, 94%) or ultrasound (10 min, 95% efficiency). The studies prove that the PTC synthesis process of ethenzamide can be conducted under mild conditions, with a shorter reaction time and remarkably lower energy consumption in comparison to conventional processes, thus actualizing “green chemistry” for practical ethenzamide preparation. Full article
(This article belongs to the Special Issue Advances in Organic Synthetic Chemistry)
24 pages, 7885 KiB  
Article
Catalytic Screening for 1,2-Diol Protection: A Saccharose-Derived Hydrothermal Carbon Showcases Enhanced Performance
by Laura Moreno, Rosario Pardo-Botello, Carlos J. Durán-Valle, Marta Adame-Pereira, Pedro Cintas, Larrisa Chan, David Cantillo and Rafael Fernando Martínez
Appl. Sci. 2025, 15(2), 807; https://doi.org/10.3390/app15020807 - 15 Jan 2025
Viewed by 818
Abstract
A benchmarking study is reported on a series of modified carbocatalysts to efficiently promote the acetalization of 1,2-diols under heterogeneous conditions. Among the catalysts surveyed, a hydrothermal carbon generated from saccharose, a cheap, abundant, and biobased material, showed excellent performance when tested on [...] Read more.
A benchmarking study is reported on a series of modified carbocatalysts to efficiently promote the acetalization of 1,2-diols under heterogeneous conditions. Among the catalysts surveyed, a hydrothermal carbon generated from saccharose, a cheap, abundant, and biobased material, showed excellent performance when tested on two representative diols. All catalysts have been thoroughly characterized, focusing on surface acidity and composition. Optimal working parameters such as temperature and catalyst loading could be established. Remarkably, sonication improved the diol protection, which proceeded faster at 25 °C. The catalyst could be easily recycled and reused several times. In addition, the protocol was successfully translated from batch to continuous flow operation using a packed-bed reactor. Full article
(This article belongs to the Special Issue Advances in Organic Synthetic Chemistry)
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13 pages, 3304 KiB  
Article
Upgrading Biomass Wastes to Graphene Quantum Dots with White-Light-Emitting Features in the Solid State
by Pierre Magri, Pascal Franchetti, Jean-Jacques Gaumet, Benoit Maxit, Sébastien Diliberto and Philippe Pierrat
Appl. Sci. 2024, 14(19), 8807; https://doi.org/10.3390/app14198807 - 30 Sep 2024
Viewed by 1092
Abstract
The emergence of bio-based carbonaceous materials for various applications has attracted significant attention during the last few years. Here, we report a rapid, efficient, and reproducible microwave-assisted synthesis of graphene quantum dots (GQDs) with identical features irrespective of the nature of biomass waste [...] Read more.
The emergence of bio-based carbonaceous materials for various applications has attracted significant attention during the last few years. Here, we report a rapid, efficient, and reproducible microwave-assisted synthesis of graphene quantum dots (GQDs) with identical features irrespective of the nature of biomass waste investigated. The synthesized GQDs were fully characterized by X-ray photoelectron spectroscopy, Fourier-transform infrared spectroscopy, transmission electron microscopy, and dynamic light scattering. The nanoparticles displayed narrow sizes of 1–2 nm and high solubility in polar solvents such as water and ethanol. The protocol described herein is advantageous in comparison to dealing with the synthesis of GQDs from biomass waste previously reported since our protocol is faster owing to the use of microwave heating and the avoidance of dialysis for the purification step. Furthermore, in solution, the water-soluble particles showed excitation-dependent photoluminescence ranging from blue to orange emission wavelengths. Interestingly, thin films displayed white-light emission under 325 nm UV-light excitation, while aggregation-induced quenching was usually observed, opening the way for their potential use as a phosphor in white-light-emitting diodes. Full article
(This article belongs to the Special Issue Advances in Organic Synthetic Chemistry)
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15 pages, 4610 KiB  
Article
Synthesis, Characterization and Biological Activity Evaluation of Some 1,N-bis-(4-amino-5-mercapto-1,2,4-triazol-3-yl) Alkanes
by Andreea-Anda Alexa, Vasile-Nicolae Bercean, Sabina Elena Boncea, Adriana Ledeţi, Valentin Badea, Amalia Ridichie, Marilena Motoc and Ionuţ Ledeţi
Appl. Sci. 2024, 14(14), 6180; https://doi.org/10.3390/app14146180 - 16 Jul 2024
Viewed by 1060
Abstract
In this paper, we present the synthesis, characterization and evaluation of antiproliferative activity for four compounds carrying the 4-amino-5-mercapto-1,2,4-triazol-3-yl scaffold. The synthesis of 1,n-bis-(4-amino-5-mercapto-1,2,4-triazol-3-yl) alkanes was carried out using as starting reagents the dihydrazides of oxalic, malonic, succinic and adipic acids, using mercaptoacetic [...] Read more.
In this paper, we present the synthesis, characterization and evaluation of antiproliferative activity for four compounds carrying the 4-amino-5-mercapto-1,2,4-triazol-3-yl scaffold. The synthesis of 1,n-bis-(4-amino-5-mercapto-1,2,4-triazol-3-yl) alkanes was carried out using as starting reagents the dihydrazides of oxalic, malonic, succinic and adipic acids, using mercaptoacetic acid dianion as a leaving group, by a one-pot synthesis method implemented in our research group for the synthesis of 3-substituted-5-mercapto-1,2,4-triazoles. The compounds were obtained with modest yields (12–60%) but with good purity and were characterized by elemental analysis, FTIR, 1H-NMR and 13C-NMR spectroscopy. Also, the stability of the synthesized bis-triazoles was investigated under controlled thermal stress in a dynamic oxidative atmosphere. The last part of the study consisted of biological activity evaluation, by evaluating the antiproliferative activity against the A375 line (human malignant melanoma), as well as on viability of the BJ fibroblast cell line, using MTT and LDH assays. Full article
(This article belongs to the Special Issue Advances in Organic Synthetic Chemistry)
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19 pages, 8911 KiB  
Article
Aromatic Amines in Organic Synthesis Part III; p-Aminocinnamic Acids and Their Methyl Esters
by Marek Pietrzak and Beata Jędrzejewska
Appl. Sci. 2024, 14(14), 6032; https://doi.org/10.3390/app14146032 - 10 Jul 2024
Viewed by 1039
Abstract
Fifteen amine derivatives of cinnamic acid were synthesized by reaction of the corresponding benzaldehydes and malonic acid. The selected acids were then converted into methyl esters. Three esterification methods were tested with (1) thionyl chloride in methanol, (2) sulfuric acid in methanol, and [...] Read more.
Fifteen amine derivatives of cinnamic acid were synthesized by reaction of the corresponding benzaldehydes and malonic acid. The selected acids were then converted into methyl esters. Three esterification methods were tested with (1) thionyl chloride in methanol, (2) sulfuric acid in methanol, and (3) dimethyl sulfate in acetone. The latter method turned out to be the best, both in terms of reaction efficiency and product purity. The chemical structure and purity of all the synthesized compounds were verified by elemental analysis, 1H and 13C NMR, and IR spectroscopy. The cinnamic acids and their esters, thanks to an extensive system of conjugated double bonds compared to analogous benzoic acids, can be used to obtain dyes for various applications, including non-linear optics and optoelectronics. Therefore, their basic spectroscopic properties are presented as well. Full article
(This article belongs to the Special Issue Advances in Organic Synthetic Chemistry)
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Review

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31 pages, 2087 KiB  
Review
Guineensine: Isolation, Synthesis, and Biological Activity
by Dimitris Matiadis, Eleni Kakouri, Eleftheria H. Kaparakou and Petros A. Tarantilis
Appl. Sci. 2025, 15(3), 1444; https://doi.org/10.3390/app15031444 - 30 Jan 2025
Viewed by 456
Abstract
The genus Piper is the largest among plants of the Piperaceae family. Phytochemical studies on various piper species indicate the presence of bioactive compounds, with alkamides being among the most prominent. Piperine is well studied, and is usually found in abundance in most [...] Read more.
The genus Piper is the largest among plants of the Piperaceae family. Phytochemical studies on various piper species indicate the presence of bioactive compounds, with alkamides being among the most prominent. Piperine is well studied, and is usually found in abundance in most species. Guineensine is an alkamide that merits particular interest and, until now, has received less scientific attention. Therefore, in the present review, we discuss guineensine’s isolation, synthesis, and pharmacological activity. Data were collected from 1974 to 2024. Databases including PubMed, Google Scholar, and Science Direct were used to retrieved information using the following keywords: guineensine, isolation, synthesis, biological activity, alkamides, Piper spp., pepper, and SAR. Guineensine is obtained using various isolation methods. However, it yields low amounts; therefore, its synthesis is important. In addition, guineensine exerts many biological activities. Its potential is connected to its terminal benzodioxolyl and isobutyamide groups and to the length of its unsaturated carbon chain of twelve atoms. Findings of the studies presented in this review provide substantiation regarding the scientific interest in guineensine. Isolation procedures present advantages and disadvantages, and the methods of its synthesis are efficient. Its biological activity seems promising and further studies may lead to the development of new therapeutic agents. Full article
(This article belongs to the Special Issue Advances in Organic Synthetic Chemistry)
41 pages, 10754 KiB  
Review
Synthesis and Characteristics of 1,2,4,5-Tetrazines for Using as High Energy Density Materials (HEDMs)
by Sebastian Górecki and Agnieszka Kudelko
Appl. Sci. 2025, 15(2), 821; https://doi.org/10.3390/app15020821 - 15 Jan 2025
Viewed by 762
Abstract
Nitrogen-rich heterocycles constitute a family of high energy density materials (HEDMs) that have been developing intensively in recent years. A representative of this class is 1,2,4,5-tetrazine, a six-membered aromatic compound containing four nitrogen atoms in the ring. Many energetic compounds with this scaffold [...] Read more.
Nitrogen-rich heterocycles constitute a family of high energy density materials (HEDMs) that have been developing intensively in recent years. A representative of this class is 1,2,4,5-tetrazine, a six-membered aromatic compound containing four nitrogen atoms in the ring. Many energetic compounds with this scaffold exhibit thermal stability, high density, and insensitivity to various stimuli, including friction, impact, and electrostatic discharge. This review presents methods for constructing 1,2,4,5-tetrazine precursors from acyclic reagents and describes their chemical modifications, leading to new energetic compounds with potential applications in the industry as explosives, propellants, or pyrotechnics. Synthetic procedures and reaction conditions are discussed, along with the detonation parameters of new nitrogen-rich tetrazine-based products, which allow estimation of their application potential. Full article
(This article belongs to the Special Issue Advances in Organic Synthetic Chemistry)
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