Issue 45, 2022, Issue in Progress

A practical flow synthesis of 1,2,3-triazoles


A robust and versatile protocol for synthesis of 1-monosubstituted and 1,4-disubstituted 1H-1,2,3-triazoles was established under continuous flow conditions using copper-on-charcoal as a heterogeneous catalyst. This methodology allowed for the synthesis of a diverse set of substituted 1,2,3-triazoles with good functional group tolerance and high yields. 2-Ynoic acids were also used as small-chain alkyne donors in a decarboxylation/cycloaddition cascade, allowing gaseous reagents to be bypassed, delivering desired triazoles in high yields. The developed methodology was used to synthesize an antiepileptic agent, rufinamide, which was obtained in 96% isolated yield.

Graphical abstract: A practical flow synthesis of 1,2,3-triazoles

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Article information

Article type
28 Jul 2022
01 Oct 2022
First published
11 Oct 2022
This article is Open Access
Creative Commons BY license

RSC Adv., 2022,12, 28910-28915

A practical flow synthesis of 1,2,3-triazoles

D. Drelinkiewicz and R. J. Whitby, RSC Adv., 2022, 12, 28910 DOI: 10.1039/D2RA04727F

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