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Copper catalysis

Rewiring amino acids to piperidines

Nature Catalysis volume 8, pages 1133–1134 (2025)Cite this article

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Bioactive piperidines are among the most common motifs in pharmaceuticals, yet accessing their chiral, highly substituted forms remains challenging. Now, a copper-catalysed reaction of amino-acid-derived cyclopropanols with aldehydes unites catalyst design with the natural chirality of reagents to access a broad family of stereodefined cis-2,6-disubstituted piperidines, expanding opportunities in drug discovery and natural product synthesis.

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Fig. 1: Stereocontrolled synthesis of cis-2,6-disubstituted piperidines via intramolecular homo-Mannich reaction.

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Authors and Affiliations

  1. Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan

    Naohiko Yoshikai

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  1. Naohiko Yoshikai
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Correspondence to Naohiko Yoshikai.

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Yoshikai, N. Rewiring amino acids to piperidines. Nat Catal 8, 1133–1134 (2025). https://doi.org/10.1038/s41929-025-01444-0

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