SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS

Amino acids are fundamental to virtually every aspect of biological science and healthcare ser­ving as the cornerstone of molecular structure and function. Research has now expanded beyond naturally occurring amino acids to tailor-made derivatives enabling precise control over biological pro­cesses...

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Бібліографічні деталі
Дата:2025
Автори: Wzorek, Alicja, Han, Jianlin, Ono, Taizo, Klika, Karel, Baecker, Daniel, Zhang, Wei, Soloshonok, Vadim
Формат: Стаття
Мова:English
Опубліковано: V.I.Vernadsky Institute of General and Inorganic Chemistry 2025
Онлайн доступ:https://ucj.org.ua/index.php/journal/article/view/745
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Назва журналу:Ukrainian Chemistry Journal

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Ukrainian Chemistry Journal
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spelling oai:ojs2.1444248.nisspano.web.hosting-test.net:article-7452025-11-25T14:50:50Z SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS Wzorek, Alicja Han, Jianlin Ono, Taizo Klika, Karel Baecker, Daniel Zhang, Wei Soloshonok, Vadim Fluorine, Amino Acids, Fluorinated Pharmaceuticals, Unsaturated/Olefinic Groups, Synthesis, Nucleophilic and Electrophilic Glycine Equivalents. Amino acids are fundamental to virtually every aspect of biological science and healthcare ser­ving as the cornerstone of molecular structure and function. Research has now expanded beyond naturally occurring amino acids to tailor-made derivatives enabling precise control over biological pro­cesses and unlocking new functionalities unattainable with standard amino acids and peptides. One of the most exciting advancements is the development of fluorine-containing amino acids which integrate the powerful pharmacological effects of fluorine with the structural adaptability of amino acid frameworks. This review explores the synthesis of fluorinated amino acids bearing unsaturated residues—a highly valuable and distinct subgroup within the broader class of fluorinated amino acids. These specialized molecules feature fluorine directly bonded to sp2-hybridized carbon atoms, effectively replicating the electronic properties of aromatic substitution without relying on an aromatic system. The olefinic placement of fluorine enhances molecular stability and imparts specific steric, geometric, chemical, and biological characteristics critical for drug design and bioactive compound development. The synthetic strategies presented herein are organized around key transformations, including α alkylation of amino acids, side chain elaboration, introduction of amino and/or carboxylic functionalities, and the generation of unsaturation within fluoro-amino acid cores. By compiling these methodologies we aim to provide a comprehensive resource and a source of inspiration for researchers engaged in synthetic and medicinal chemistry, drug discovery, and organofluorine chemistry. V.I.Vernadsky Institute of General and Inorganic Chemistry 2025-09-25 Article Article Organic chemistry Органическая xимия Органічна xімія application/pdf https://ucj.org.ua/index.php/journal/article/view/745 10.33609/2708-129X.91.8.2025.36-64 Ukrainian Chemistry Journal; Vol. 91 No. 8 (2025): Ukrainian Chemistry Journal; 36-64 Украинский химический журнал; Том 91 № 8 (2025): Ukrainian Chemistry Journal; 36-64 Український хімічний журнал; Том 91 № 8 (2025): Ukrainian Chemistry Journal; 36-64 2708-129X 2708-1281 en https://ucj.org.ua/index.php/journal/article/view/745/382
institution Ukrainian Chemistry Journal
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datestamp_date 2025-11-25T14:50:50Z
collection OJS
language English
topic_facet Fluorine
Amino Acids
Fluorinated Pharmaceuticals
Unsaturated/Olefinic Groups
Synthesis
Nucleophilic and Electrophilic Glycine Equivalents.
format Article
author Wzorek, Alicja
Han, Jianlin
Ono, Taizo
Klika, Karel
Baecker, Daniel
Zhang, Wei
Soloshonok, Vadim
spellingShingle Wzorek, Alicja
Han, Jianlin
Ono, Taizo
Klika, Karel
Baecker, Daniel
Zhang, Wei
Soloshonok, Vadim
SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS
author_facet Wzorek, Alicja
Han, Jianlin
Ono, Taizo
Klika, Karel
Baecker, Daniel
Zhang, Wei
Soloshonok, Vadim
author_sort Wzorek, Alicja
title SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS
title_short SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS
title_full SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS
title_fullStr SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS
title_full_unstemmed SYNTHESIS OF TAILOR-MADE AMINO ACIDS CONTAINING C(sp2)–F BONDS
title_sort synthesis of tailor-made amino acids containing c(sp2)–f bonds
description Amino acids are fundamental to virtually every aspect of biological science and healthcare ser­ving as the cornerstone of molecular structure and function. Research has now expanded beyond naturally occurring amino acids to tailor-made derivatives enabling precise control over biological pro­cesses and unlocking new functionalities unattainable with standard amino acids and peptides. One of the most exciting advancements is the development of fluorine-containing amino acids which integrate the powerful pharmacological effects of fluorine with the structural adaptability of amino acid frameworks. This review explores the synthesis of fluorinated amino acids bearing unsaturated residues—a highly valuable and distinct subgroup within the broader class of fluorinated amino acids. These specialized molecules feature fluorine directly bonded to sp2-hybridized carbon atoms, effectively replicating the electronic properties of aromatic substitution without relying on an aromatic system. The olefinic placement of fluorine enhances molecular stability and imparts specific steric, geometric, chemical, and biological characteristics critical for drug design and bioactive compound development. The synthetic strategies presented herein are organized around key transformations, including α alkylation of amino acids, side chain elaboration, introduction of amino and/or carboxylic functionalities, and the generation of unsaturation within fluoro-amino acid cores. By compiling these methodologies we aim to provide a comprehensive resource and a source of inspiration for researchers engaged in synthetic and medicinal chemistry, drug discovery, and organofluorine chemistry.
publisher V.I.Vernadsky Institute of General and Inorganic Chemistry
publishDate 2025
url https://ucj.org.ua/index.php/journal/article/view/745
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last_indexed 2025-12-02T15:13:46Z
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