Pyrazoles: 'one-pot' synthesis from arenes and carboxylic acids

Org Biomol Chem. 2020 Aug 7;18(29):5625-5638. doi: 10.1039/d0ob01228a. Epub 2020 Jul 10.

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.

Publication types

  • Research Support, Non-U.S. Gov't