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DOI: 10.1055/s-0042-2051
Asymmetric Synthesis of 2-Arylethylamines: 2025. An Updated Review
Authors
The authors gratefully acknowledge the financial support for this work provided by Ministerio de Ciencia e Innovación (PID2020-118303GB-I00 and MCIN/AEI/10.13039/501100011033), Junta de Castilla y León (SA076P20) and Universidad de Salamanca (Programme I, GIR PRONABIOLACT).
Abstract
2-Arylethylamines are present in several natural bioactive compounds, as well as in many nitrogen-containing drugs. Their ability to cross the blood–brain barrier makes this family of compounds of special interest in medicinal chemistry. Asymmetric methodologies towards the synthesis of 2-arylethylamine motifs are of significant interest due to the challenges they present. In this graphical review, we highlight recent advances in the metal-free and metal-catalyzed asymmetric synthesis of 2-arylethylamines, covering the literature published in 2025 (up until late October). We showcase the different methodologies towards the aforementioned motif, including chiral induction, organocatalysis, organophotocatalysis and enzymatic catalysis.
Key words
2-phenethylamines - 2-arylethylamines - asymmetric synthesis - chiral induction - organocatalysis - organophotocatalysis - enzymatic catalysis - metal catalysisPublication History
Received: 27 October 2025
Accepted after revision: 03 December 2025
Article published online:
18 December 2025
© 2025. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by/4.0/)
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