Pyrazoles: ‘one-pot’ synthesis from arenes and carboxylic acids?

Organic & Biomolecular Chemistry Pub Date: 2020-06-30 DOI: 10.1039/D0OB01228A

Abstract

A rapid and efficient method for ‘one-pot’ synthesis of pyrazoles from (hetero)arenes and carboxylic acids via successive formation of ketones and β-diketones followed by heterocyclization with hydrazine has been developed. The utility of the RCOOH/TfOH/TFAA acylation system for intermediate production of ketones and 1,3-diketones is a key feature of this approach. The preliminary evaluation of the anticancer activity of the synthesized pyrazoles is performed.

Graphical abstract: Pyrazoles: ‘one-pot’ synthesis from arenes and carboxylic acids
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