Synthesis of new triazole-based trifluoromethyl scaffolds

Beilstein J Org Chem. 2008:4:19. doi: 10.3762/bjoc.4.19. Epub 2008 May 29.

Abstract

Trifluoromethyl propargylamines react with various azide derivatives to afford 1,4-disubstituted 1,2,3-triazoles through a Huisgen 1,3-dipolar cycloaddition. The reaction is catalyzed by a Cu(I) species in acetonitrile, and the corresponding products are obtained in good yields. This process thus offers an entry to new trifluoromethyl peptidomimetics as interesting scaffolds.

Keywords: catalysis; click chemistry; copper; fluorine; heterocycle; peptidomimetics.