Preparation of new gem-difluoro heterocyclic-fused 1,2,3-triazole derivatives |
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Authors: | Layal Hariss Zeinab Barakat Farès Farès Thierry Roisnel René Grée Ali Hachem |
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Institution: | 1. Laboratory for Medicinal Chemistry and Natural Products, Lebanese University, Faculty of Sciences (1) and PRASE-EDST, Hadath, Beirut, Lebanon;2. Univ Rennes, CNRS ISCR (Institut des Sciences Chimiques de Rennes), UMR 6226, F-35000 Rennes, France |
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Abstract: | Starting from easily accessible gem-difluoropropargylic derivatives a cascade nucleophilic substitution by N3–, followed by an intramolecular 1,3 dipolar cycloaddition, afforded in fair to good yields new 1,2,3-triazoles fused to pyrrolidines or piperidines. These molecules, with a gem-difluoro group vicinal to the triazoles, are fluorinated analogues of bioactive heterocycles. In parallel, a few open chain analogues have been prepared in order to evaluate the possible role of the bicyclic core on the biological properties of such molecules. |
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Keywords: | Fluorine Propargylic fluorides Triazoles Heterocycles 1 3 Dipolar cycloaddition |
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