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Multi-gram scale mercury-free synthesis of optically pure 3,4,5-trisubstituted 1,2,4-triazoles using silver benzoate
Journal article   Peer reviewed

Multi-gram scale mercury-free synthesis of optically pure 3,4,5-trisubstituted 1,2,4-triazoles using silver benzoate

Mathieu Bibian, Anne-Laure Blayo, Aline Moulin, Jean Martinez and Jean-Alain Fehrentz
Tetrahedron Letters, Vol.51(19), pp.2660-2663
2010
DOI: https://doi.org/10.1016/j.tetlet.2010.03.037

Abstract

heterocycles silver 4-triazole scale-up enantiopure pharmacological in-vitro ghrelin receptor vivo evaluations triazole derivatives inhibitors antagonists ligands 0040-4039
We report a new method using silver benzoate instead of mercury salts as a key reagent for the synthesis of 3,4,5-trisubstituted 1,2,4-triazoles. This method allows the introduction of a large variety of substituents in the three positions. We demonstrated that we could introduce one chiral center without any loss of the optical purity. This method is compatible with at least multi-gram scale-up. (C) 2010 Elsevier Ltd. All rights reserved.
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