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Synthesis 2011(17): 2733-2736  
DOI: 10.1055/s-0030-1260103
SPECIALTOPIC
© Georg Thieme Verlag Stuttgart ˙ New York

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;
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Publication History

Received 25 February 2011
Publication Date:
08 July 2011 (online)

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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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