European Journal of Organic Chemistry · 2021 · 18 citations · 77 references
Natural SciencesChemistryMedicinal ChemistryDrug DiscoveryOrganic ChemistrySynthetic Medicinal ChemistryHalogen ChemistryHeterocycle SynthesisHeterocyclic ChemistryHeterocyclic CompoundsTriazole ChemistryTriazole Synthesis
Abstract 1,2,3‐triazoles are important scaffolds in several fields, and there is still a demand to construct these compounds, most notably the disubstituted 4, 5 compounds. The latter are obtained in different ways, but the 4‐ and 5‐halo triazoles are generally the key intermediates in their synthesis. These halogenated compounds are an extraordinary platform leading to a great chemical diversity around the 4 and 5 positions. However, their own pathways are generally put aside at the expense of the substituted triazoles. This review is focused on the main synthesis of 5‐ and 4‐halo 1,2,3‐triazoles from cycloaddition followed or not by halogenation reaction. Unlike the halogens (iodine, bromine, and chlorine), the 5‐ and 4‐fluoro 1,2,3‐triazoles will be presented separately due to their relatively more difficult and still recently challenging synthesis.
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Christian W. Tornøe, Caspar Christensen, Morten Meldal · The Journal of Organic Chemistry · 2002 · 8.5K citations
Polytriazoles as Copper(I)-Stabilizing Ligands in Catalysis
Timothy R. Chan, Robert Hilgraf, K. Barry Sharpless et al. · Organic Letters · 2004 · 1.5K citations
Folkert Reck, Fei Zhou, Marc Girardot et al. · Journal of Medicinal Chemistry · 2005 · 326 citations · Full text