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Current Development of Asymmetric Catalysis and Synthesis
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Current Development of Asymmetric Catalysis and Synthesis

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 7879

Special Issue Editor

Prof. Dr. Jiaxi Xu

E-Mail Website
Guest Editor
Department of Organic Chemistry, Faculty of Science, Beijing University of Chemical Technology, Beijing 100029, China
Interests: synthetic methodology; asymmetric synthesis and catalysis; heterocycles; taurines; peptide chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Enantiopure organic compounds are important in both biological and medicinal chemistry and material chemistry. Most medicines are optically active compounds. Asymmetric catalysis and synthesis are efficient methods for the preparation of optically active organic compounds and have been well developed over the last three decades. Various optically active chiral catalysts and asymmetric reactions have been achieved and applied.

This Special Issue of Molecules welcomes leading scientists to submit original research papers and reviews in the fields of asymmetric catalysis and synthesis, including asymmetric synthesis, asymmetric catalysis, transition metal-catalyzed asymmetric catalysis and synthesis, organocatalyzed asymmetric catalysis and synthesis, enzyme-catalyzed catalysis and synthesis, kinetic resolution, theoretical investigations into asymmetric catalysis and synthesis, chemical modification of chiral organic compounds, and their related biological activity. Potential topics include, but are not limited to, the keywords listed below.

Prof. Dr. Jiaxi Xu
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. 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

  • asymmetric synthesis
  • asymmetric catalysis
  • transition metal-catalyzed asymmetric catalysis and synthesis
  • organocatalyzed asymmetric catalysis and synthesis
  • enzyme-catalyzed catalysis and synthesis
  • kinetic resolution
  • theoretical investigations into asymmetric catalysis and synthesis

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Related Special Issue

Published Papers (6 papers)

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Research

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16 pages, 2404 KiB  
Article
Squaramide-Catalyzed Asymmetric Michael Addition/Cyclization Reaction for the Synthesis of Chiral Bisspiro Barbituric Acid–Oxindole Derivatives
by De-Jun Qiao and Da-Ming Du
Molecules 2025, 30(9), 2000; https://doi.org/10.3390/molecules30092000 - 30 Apr 2025
Abstract
An efficient stereoselective strategy for the synthesis of chiral bisspiro barbituric acid–oxindole derivatives was developed. The asymmetric Michael addition/cyclization tandem reaction between benzylidene barbituric acids and oxindolylmalonitriles was catalyzed by squaramide catalyst, and the corresponding spirocyclic products were obtained in good-to-high yields (up [...] Read more.
An efficient stereoselective strategy for the synthesis of chiral bisspiro barbituric acid–oxindole derivatives was developed. The asymmetric Michael addition/cyclization tandem reaction between benzylidene barbituric acids and oxindolylmalonitriles was catalyzed by squaramide catalyst, and the corresponding spirocyclic products were obtained in good-to-high yields (up to 97%) with excellent stereoselectivities (up to >99% ee, >20:1 dr). At the same time, the practicality of the reaction was verified by the gram-scale preparation reaction. Full article
(This article belongs to the Special Issue Current Development of Asymmetric Catalysis and Synthesis)
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11 pages, 1006 KiB  
Article
Enantioselective Synthesis of the Sex Pheromone of Sitodiplosis mosellana (Géhin) and Its Stereoisomers
by Jianan Wang, Xiaoyang Li, Yun Zhou, Qinghua Bian and Jiangchun Zhong
Molecules 2025, 30(3), 671; https://doi.org/10.3390/molecules30030671 - 3 Feb 2025
Viewed by 630
Abstract
(2S,7S)-2,7-Nonanediyl dibutyrate is the sex pheromone of Sitodiplosis mosellana (Géhin). In this study, this sex pheromone and its three stereoisomers were prepared. Central to this strategy was the ring opening of chiral epoxide with an alkynyllithium and the hydrogenation [...] Read more.
(2S,7S)-2,7-Nonanediyl dibutyrate is the sex pheromone of Sitodiplosis mosellana (Géhin). In this study, this sex pheromone and its three stereoisomers were prepared. Central to this strategy was the ring opening of chiral epoxide with an alkynyllithium and the hydrogenation of the triple bond. Moreover, this approach consisted of six steps, and the total yields were 59–64%. Full article
(This article belongs to the Special Issue Current Development of Asymmetric Catalysis and Synthesis)
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16 pages, 2654 KiB  
Article
PyBox–La(OTf)3-Catalyzed Enantioselective Diels–Alder Cycloadditions of 2-Alkenoylpyridines with Cyclopentadiene
by Hao Wei, Yujie Zhang, Sanlin Jin, Ying Yu, Ning Chen, Jiaxi Xu and Zhanhui Yang
Molecules 2024, 29(13), 2978; https://doi.org/10.3390/molecules29132978 - 22 Jun 2024
Cited by 1 | Viewed by 1588
Abstract
The PyBox–La(OTf)3-catalyzed enantioselective Diels–Alder cycloaddition of 2-alk-2-enoylpyridines with cyclopentadiene is realized, producing enantiopure disubstituted norbornenes, which possess four contiguous stereocenters and are biologically relevant structures in up to 92:8 dr and 99:1 er. Full article
(This article belongs to the Special Issue Current Development of Asymmetric Catalysis and Synthesis)
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Review

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64 pages, 42508 KiB  
Review
Transition Metal Catalysis for the Asymmetric Synthesis of 2-Arylethylamines: A Review of the New Millennium
by Alejandro Manchado, Ángel García-González, Carlos T. Nieto, Nieves G. Ledesma, David Díez and Narciso M. Garrido
Molecules 2025, 30(8), 1721; https://doi.org/10.3390/molecules30081721 - 11 Apr 2025
Viewed by 215
Abstract
The 2-arylethylamine motif is very well-known in medicinal chemistry because of its interesting properties when it comes to interacting with the Central Neural System thanks to its ability to pass the blood–brain barrier. This nitrogen-containing family of compounds is of great interest in [...] Read more.
The 2-arylethylamine motif is very well-known in medicinal chemistry because of its interesting properties when it comes to interacting with the Central Neural System thanks to its ability to pass the blood–brain barrier. This nitrogen-containing family of compounds is of great interest in synthetic organic chemistry and, when it comes to its asymmetric synthesis, great challenges can be faced in order to obtain the chiral purity required in the drug industry. Thus, we provide a concise transition metal review presenting the recent advances in the synthesis of chiral 2-arylethylamines using transition metals as the main catalysts in the introduction of chirality. Both conventional and photocatalysis methods will be covered, considering the main transition metal used in the studies. Full article
(This article belongs to the Special Issue Current Development of Asymmetric Catalysis and Synthesis)
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20 pages, 6221 KiB  
Review
Recent Advances in the Utilization of Chiral Covalent Organic Frameworks for Asymmetric Photocatalysis
by Peng Liu, Weijun Dai, Xianfu Shen, Xiang Shen, Yuxiang Zhao and Jian-Jun Liu
Molecules 2024, 29(21), 5006; https://doi.org/10.3390/molecules29215006 - 23 Oct 2024
Cited by 2 | Viewed by 1702
Abstract
The use of light energy to drive asymmetric organic transformations to produce high-value-added organic compounds is attracting increasing interest as a sustainable strategy for solving environmental problems and addressing the energy crisis. Chiral covalent organic frameworks (COFs), as porous crystalline chiral materials, have [...] Read more.
The use of light energy to drive asymmetric organic transformations to produce high-value-added organic compounds is attracting increasing interest as a sustainable strategy for solving environmental problems and addressing the energy crisis. Chiral covalent organic frameworks (COFs), as porous crystalline chiral materials, have become an important platform on which to explore new chiral photocatalytic materials due to their precise tunability, chiral structure, and function. This review highlights recent research progress on chiral COFs and their crystalline composites, evaluating their application as catalysts in asymmetric photocatalytic organic transformations in terms of their structure. Finally, the limitations and challenges of chiral COFs in asymmetric photocatalysis are discussed, with future opportunities for research being identified. Full article
(This article belongs to the Special Issue Current Development of Asymmetric Catalysis and Synthesis)
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27 pages, 4302 KiB  
Review
Recent Advances in π-Stacking Interaction-Controlled Asymmetric Synthesis
by Jiaxi Xu
Molecules 2024, 29(7), 1454; https://doi.org/10.3390/molecules29071454 - 24 Mar 2024
Cited by 5 | Viewed by 3227
Abstract
The π-stacking interaction is one of the most important intramolecular and intermolecular noncovalent interactions in organic chemistry. It plays an important role in stabilizing some structures and transition states in certain reactions via both intramolecular and intermolecular interactions, facilitating different selectivities, such as [...] Read more.
The π-stacking interaction is one of the most important intramolecular and intermolecular noncovalent interactions in organic chemistry. It plays an important role in stabilizing some structures and transition states in certain reactions via both intramolecular and intermolecular interactions, facilitating different selectivities, such as chemo-, regio-, and stereoselectivities. This minireview focuses on the recent examples of the π-stacking interaction-controlled asymmetric synthesis, including auxiliary-induced asymmetric synthesis, kinetic resolution, asymmetric synthesis of helicenes and heterohelicenes, and multilayer 3D chiral molecules. Full article
(This article belongs to the Special Issue Current Development of Asymmetric Catalysis and Synthesis)
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