TFA-promoted (hetero)arylation/hydroxylation of quinoxaline-2-one derivatives with electron-rich aromatic compounds

Ramanna Jatoth; Kishan Gugulothu; Nidhi Ravi; Ranamalla Gayathri; Shravani Parehosahalli Chandrakumar; K Shiva Kumar

doi:10.1039/d4ob00882k

TFA-promoted (hetero)arylation/hydroxylation of quinoxaline-2-one derivatives with electron-rich aromatic compounds

Org Biomol Chem. 2025 Jan 2;23(2):313-317. doi: 10.1039/d4ob00882k.

Authors

Ramanna Jatoth¹, Kishan Gugulothu¹, Nidhi Ravi², Ranamalla Gayathri², Shravani Parehosahalli Chandrakumar², K Shiva Kumar^{1

2}

Affiliations

¹ Department of Chemistry, Osmania University, Hyderabad-500 007, India. shivakumarkota@yahoo.co.in.
² Department of Chemistry, School of Physical Sciences, Central University of Kerala, Kasaragod, Kerala 671320, India.

PMID: 39589367
DOI: 10.1039/d4ob00882k

Abstract

A metal- and solvent-free, one-pot and TFA-promoted method for the construction of hetero/aryl-substituted quinoxalin-2-ones, pyrazin-2(1H)-ones, and pyrimidin-4(3H)-ones is reported. This method involves the reaction of chloro-derivatives of nitrogen heterocycles with electron-rich arenes/heteroarenes, followed by hydroxylation. This protocol is easy to use, providing access to (hetero)aryl-substituted N-heterocycles in good yields.