Advances in the Synthetic Approaches to α‐Amino Ketones: Scope, Mechanism, and Application

α‐amino ketones (α‐AKs) serve as valuable building blocks in synthetic and medicinal chemistry because they are found in many pharmaceuticals and molecules that are biologically active. Different catalytic strategies for their synthesis have been developed as a result of their structural diversity and functional versatility. This review offers a thorough summary of recent developments (2020–2025) in the catalytic synthesis of α‐AKs, emphasizing two main categories: enantioselective (chiral) and achiral methods. Chiral techniques, which offer high enantioselectivity and wide substrate scopes, include transition metal catalysis, organocatalysis, photoredox catalysis, and their combinations. Despite being simpler and more scalable, chiral strategies are useful for quickly building α‐AK scaffolds. With a focus on reaction design, mechanism, tolerance to functional groups, and synthetic utility, recent synthetic approaches are discussed. In addition to outlining the opportunities and challenges that lie ahead in extending the synthetic accessibility and application of these privileged molecular architectures, the review highlights the advancements that have been made in both fields.

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Publication Details

Journal
European Journal of Organic Chemistry
Published
2026-01-04
DOI
https://doi.org/10.1002/ejoc.202501074
Primary Topic
Asymmetric Synthesis and Catalysis
Type
article
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0.00
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article

Advances in the Synthetic Approaches to α‐Amino Ketones: Scope, Mechanism, and Application

Elizabeth J. Diana, Thomas Mathew, Jisna Jose
European Journal of Organic Chemistry
Asymmetric Synthesis and Catalysis
article

Advances in the Synthetic Approaches to α‐Amino Ketones: Scope, Mechanism, and Application

Elizabeth J. Diana, Thomas Mathew, Jisna Jose
article en

Abstract

α‐amino ketones (α‐AKs) serve as valuable building blocks in synthetic and medicinal chemistry because they are found in many pharmaceuticals and molecules that are biologically active. Different catalytic strategies for their synthesis have been developed as a result of their structural diversity and functional versatility. This review offers a thorough summary of recent developments (2020–2025) in the catalytic synthesis of α‐AKs, emphasizing two main categories: enantioselective (chiral) and achiral methods. Chiral techniques, which offer high enantioselectivity and wide substrate scopes, include transition metal catalysis, organocatalysis, photoredox catalysis, and their combinations. Despite being simpler and more scalable, chiral strategies are useful for quickly building α‐AK scaffolds. With a focus on reaction design, mechanism, tolerance to functional groups, and synthetic utility, recent synthetic approaches are discussed. In addition to outlining the opportunities and challenges that lie ahead in extending the synthetic accessibility and application of these privileged molecular architectures, the review highlights the advancements that have been made in both fields.

European Journal of Organic ChemistryVol. 29(6)
Government Medical College (IN), Thomas College (US)
Openalex Percentile: Top 97%
Asymmetric Synthesis and Catalysis
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