# Tandem Cu(I)-Catalyzed Dipolar Cycloaddition–C–H Activation for the In-Flow Synthesis of N-Pyridyl-5-amino-1,2,3-triazole-4-carboxylates

**Authors:** Emanuela Donato, Martha C. Mayorquín-Torres, Alessandra Puglisi, Maurizio Benaglia, Mauro F. A. Adamo, Christian V. Stevens

PMC · DOI: 10.1021/acs.orglett.5c00453 · Organic Letters · 2025-04-18

## TL;DR

Scientists developed a continuous flow method to efficiently synthesize complex organic molecules using copper-catalyzed reactions.

## Contribution

A new continuous flow synthesis method combining CuAAC and C–H activation is introduced for making triazole derivatives.

## Key findings

- The process uses a packed bed reactor for efficient Cu(I)-catalyzed reactions.
- The method enables environmentally friendly synthesis of functionalized organic molecules.
- The approach combines click chemistry with C–H activation in a single setup.

## Abstract

A telescoped process under continuous flow conditions
is described
for the synthesis of N-pyridyl-5-amino-1,2,3-triazole-4-carboxylate
derivatives catalyzed by copper salts in a packed bed reactor. The
synthetic approach takes first advantage of click chemistry, specifically
relying on Cu(I)-catalyzed 1,3-dipolar azide–alkyne cycloaddition
(CuAAC), to achieve the efficient and selective assembly of a triazole
ring, followed by a copper-mediated C–H activation, that substitutes
an inert C–H bond with a C–N bond, providing an environmentally
acceptable and cost-effective strategy for synthesizing highly functionalized
organic molecules.

## Full text

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## Figures

6 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12068680/full.md

## References

25 references — full list in the complete paper: https://tomesphere.com/paper/PMC12068680/full.md

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Source: https://tomesphere.com/paper/PMC12068680