Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of Glycomimetics

1,3-Dipolar cycloadditions on nitrone dipoles are key reactions to access five-membered heterocycles, which are useful intermediates in the synthesis of biologically relevant glycomimetics. The good atomic balance and high stereoselectivity characteristic of such reactions make them good candidates...

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Main Authors: Debora Pratesi, Alessio Morano, Andrea Goti, Francesca Cardona, Camilla Matassini
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Reactions
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Online Access:https://www.mdpi.com/2624-781X/6/2/36
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author Debora Pratesi
Alessio Morano
Andrea Goti
Francesca Cardona
Camilla Matassini
author_facet Debora Pratesi
Alessio Morano
Andrea Goti
Francesca Cardona
Camilla Matassini
author_sort Debora Pratesi
collection DOAJ
description 1,3-Dipolar cycloadditions on nitrone dipoles are key reactions to access five-membered heterocycles, which are useful intermediates in the synthesis of biologically relevant glycomimetics. The good atomic balance and high stereoselectivity characteristic of such reactions make them good candidates for the development of green protocols. In the present work, these features were maximized by avoiding the use of organic solvents and considering starting materials derived from biomass. Reactions involving (acyclic and cyclic) carbohydrate-derived nitrones as dipoles and levoglucosenone as dipolarophile were considered. Performing selected 1,3-dipolar cycloadditions in neat conditions showed reduced reaction times, maintaining similar selectivity and yields with respect to the classical protocols. The use of microwave irradiation and orbital shaking were also exploited to increase the sustainability of the synthetic protocols. The collected results highlight the potential of solvent-free 1,3-dipolar cycloadditions in the design of efficient synthetic routes according to green chemistry principles, such as prevention, atom economy, safer solvents and auxiliaries, and use of renewable feedstocks.
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spelling doaj-art-d8d9edb7c93641fc857fa2cc06e5b97d2025-08-20T03:29:44ZengMDPI AGReactions2624-781X2025-06-01623610.3390/reactions6020036Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of GlycomimeticsDebora Pratesi0Alessio Morano1Andrea Goti2Francesca Cardona3Camilla Matassini4Dipartimento di Chimica “Ugo Schiff” (DICUS), Università di Firenze, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino, FI, ItalyDipartimento di Chimica “Ugo Schiff” (DICUS), Università di Firenze, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino, FI, ItalyDipartimento di Chimica “Ugo Schiff” (DICUS), Università di Firenze, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino, FI, ItalyDipartimento di Chimica “Ugo Schiff” (DICUS), Università di Firenze, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino, FI, ItalyDipartimento di Chimica “Ugo Schiff” (DICUS), Università di Firenze, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino, FI, Italy1,3-Dipolar cycloadditions on nitrone dipoles are key reactions to access five-membered heterocycles, which are useful intermediates in the synthesis of biologically relevant glycomimetics. The good atomic balance and high stereoselectivity characteristic of such reactions make them good candidates for the development of green protocols. In the present work, these features were maximized by avoiding the use of organic solvents and considering starting materials derived from biomass. Reactions involving (acyclic and cyclic) carbohydrate-derived nitrones as dipoles and levoglucosenone as dipolarophile were considered. Performing selected 1,3-dipolar cycloadditions in neat conditions showed reduced reaction times, maintaining similar selectivity and yields with respect to the classical protocols. The use of microwave irradiation and orbital shaking were also exploited to increase the sustainability of the synthetic protocols. The collected results highlight the potential of solvent-free 1,3-dipolar cycloadditions in the design of efficient synthetic routes according to green chemistry principles, such as prevention, atom economy, safer solvents and auxiliaries, and use of renewable feedstocks.https://www.mdpi.com/2624-781X/6/2/361,3-dipolar cycloadditionsnitronesglycomimeticscarbohydrateslevoglucosenonestereoselective syntheses
spellingShingle Debora Pratesi
Alessio Morano
Andrea Goti
Francesca Cardona
Camilla Matassini
Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of Glycomimetics
Reactions
1,3-dipolar cycloadditions
nitrones
glycomimetics
carbohydrates
levoglucosenone
stereoselective syntheses
title Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of Glycomimetics
title_full Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of Glycomimetics
title_fullStr Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of Glycomimetics
title_full_unstemmed Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of Glycomimetics
title_short Solvent-Free 1,3-Dipolar Cycloadditions of Nitrones for a More Sustainable Synthesis of Glycomimetics
title_sort solvent free 1 3 dipolar cycloadditions of nitrones for a more sustainable synthesis of glycomimetics
topic 1,3-dipolar cycloadditions
nitrones
glycomimetics
carbohydrates
levoglucosenone
stereoselective syntheses
url https://www.mdpi.com/2624-781X/6/2/36
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AT andreagoti solventfree13dipolarcycloadditionsofnitronesforamoresustainablesynthesisofglycomimetics
AT francescacardona solventfree13dipolarcycloadditionsofnitronesforamoresustainablesynthesisofglycomimetics
AT camillamatassini solventfree13dipolarcycloadditionsofnitronesforamoresustainablesynthesisofglycomimetics