Synthesis of 1,2,3-Triazole
Elements in Histamine H3 Receptor Ligands

Miriam Walter; Tim Kottke; Lilia Weizel; J. Stephan Schwed; Holger Stark

doi:10.1055/s-0030-1260103

SPECIALTOPIC

Synthesis of 1,2,3-Triazole Elements in Histamine H₃ Receptor Ligands

Miriam Walter, Tim Kottke, Lilia Weizel, J. Stephan Schwed, Holger Stark*
Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biocenter, ZAFES/OSF/NeFF/CMP/ICNF, Max-von-Laue-Str. 9, 60438 Frankfurt, Germany
Fax: +49(69)79829352; e-Mail: h.stark@pharmchem.uni-frankfurt.de;

Abstract

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Abstract

1,2,3-Triazole moieties were introduced in a histamine H₃ receptor antagonist pharmacophore blueprint with a versatile click chemistry approach, yielding potent ligands. Azide and alkynes were combined under copper(I) catalysis to provide the triazole element. Conventional synthesis, as well as microwave irradiation, was successfully applied.

Key words

azides - alkynes - copper catalysis - click chemistry - histamine H₃ receptor

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Referenzen

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Synthesis of 1,2,3-Triazole Elements in Histamine H3 Receptor Ligands

Synthesis of 1,2,3-Triazole Elements in Histamine H₃ Receptor Ligands