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Synfacts 2007(4): 0360-0360  
DOI: 10.1055/s-2007-968377
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart · New York

A Cu-Catalyzed C-N Bond Coupling Route to Substituted Indazoles

Contributor(s): Victor Snieckus, Oluwole Familoni
D. Viña, E. del Olmo, J. L. López-Pérez, A. San Feliciano
CIETUS, Salamanca, Spain
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Publication History

Publication Date:
23 March 2007 (online)

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Significance

A general methodology for the synthesis of indazoles based on a traditional Ullmann reaction is reported. Thus, copper-catalyzed C-N bond coupling of ortho-halo aromatic ketones and carboxylic acids with hydrazines leads to intermediates which undergo dehydration to indazoles in poor to very good yields depending on structural variation. The scope of the reaction was insufficiently investigated.