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  • Title: Rapid Access to 3-Aminoindazoles from Tertiary Amides.
    Author: Cyr P, Régnier S, Bechara WS, Charette AB.
    Journal: Org Lett; 2015 Jul 17; 17(14):3386-9. PubMed ID: 26154712.
    Abstract:
    A two-step synthesis of structurally diverse 3-aminoindazoles from readily available starting materials was developed. This sequence includes a one-pot synthesis of aminohydrazones through chemoselective Tf2O-mediated activation of tertiary amides and subsequent addition of nucleophilic hydrazides. These precursors then participate in an intramolecular ligand-free Pd-catalyzed C-H amination reaction. The azaheterocycles synthesized via this approach were further diversified through subsequent deprotection/functionalization reactions.
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