# Harnessing nitroarenes as nitrogen and oxygen sources for general oxo-aminomethylation of alkenes

**Authors:** Ting Zhou, Jing Nie, Chi Wai Cheung, Jun-An Ma

PMC · DOI: 10.1038/s41467-025-64957-z · Nature Communications · 2025-11-14

## TL;DR

This paper introduces a new method to efficiently create 3-arylamino alcohols using nitroarenes as nitrogen and oxygen sources, offering a practical and cost-effective approach for drug development.

## Contribution

The novel use of nitroarenes as dual nitrogen and oxygen sources in a metallaphotoredox-catalyzed reaction for oxo-aminomethylation of alkenes.

## Key findings

- The method provides a modular and cost-effective route to diverse 3-arylamino alcohols.
- It features broad substrate scope, excellent functional group tolerance, and high regioselectivity.
- The resulting amino alcohols can be further derivatized to enhance molecular complexity.

## Abstract

Amino alcohols are essential synthetic building blocks and privileged motifs in drug development, playing a crucial role in modulating pharmacokinetics and biological activity. However, the efficient synthesis of 3-amino alcohols remains challenging compared to their 2-amino counterparts, often requiring multistep procedures, expensive substrates, or highly sensitive reagents. Despite their versatile reactivity in advanced synthesis, nitroarenes remain underutilized as dual nitrogen and oxygen sources. Herein, we report a metallaphotoredox-catalyzed multicomponent oxo-aminomethylation of nitroarenes, tertiary alkylamines, and alkenes, providing a modular and cost-effective route to diverse 3-arylamino alcohols. This strategy features a broad substrate scope, excellent functional group tolerance, and high regioselectivity. The resulting amino alcohols serve as key intermediates for further derivatization, enhancing molecular complexity. By expanding the synthetic utility of nitroarenes, this method offers a practical and efficient pathway to bioactive molecules with pharmaceutical relevance.

Herein, the authors report a metallaphotoredox-catalyzed multicomponent oxo-aminomethylation of nitroarenes, tertiary alkylamines, and alkenes, providing a modular and cost-effective route to diverse 3-arylamino alcohols.

## Linked entities

- **Chemicals:** alkenes (PubChem CID 32932)

## Full-text entities

- **Chemicals:** nitrogen (MESH:D009584), alkenes (MESH:D000475), oxygen (MESH:D010100), Amino alcohols (MESH:D000605), 3-amino alcohols (-)

## Full text

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## Figures

9 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12618553/full.md

## References

3 references — full list in the complete paper: https://tomesphere.com/paper/PMC12618553/full.md

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Source: https://tomesphere.com/paper/PMC12618553