Preparation of new gem-difluoro heterocyclic-fused 1,2,3-triazole derivatives
2019
Abstract Starting from easily accessible gem -difluoropropargylic derivatives a cascade nucleophilic substitution by N 3 – , 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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