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;
Further Information

Publication History

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

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.

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