Issue 34, 2025

Ruthenium-catalyzed C(sp2)–H ortho-heteroarylation of 2-arylphthalazin-1(2H)-one using five-membered heteroarenes by cross-dehydrogenative coupling

Abstract

The cross-dehydrogenative coupling reactions have gained supreme importance owing to their synthetic efficiency in accessing simple to complex organic molecules. Herein, we report a Ru(II)-catalyzed directing group-assisted CDC reaction between 2-arylphthalazin-1(2H)-one and heteroarenes. This methodology offers advantages such as excellent regio-selectivity with good functional group compatibility, resulting in a broad substrate scope. Mechanistically, Ru(II)-catalyzed ortho-C(sp2)–H cross-coupling operates via a concerted metalation–deprotonation (CMD) mechanism.

Graphical abstract: Ruthenium-catalyzed C(sp2)–H ortho-heteroarylation of 2-arylphthalazin-1(2H)-one using five-membered heteroarenes by cross-dehydrogenative coupling

Supplementary files

Article information

Article type
Communication
Submitted
09 Jul 2025
Accepted
29 Jul 2025
First published
30 Jul 2025

Org. Biomol. Chem., 2025,23, 7714-7718

Ruthenium-catalyzed C(sp2)–H ortho-heteroarylation of 2-arylphthalazin-1(2H)-one using five-membered heteroarenes by cross-dehydrogenative coupling

A. Ramkumar and T. Gandhi, Org. Biomol. Chem., 2025, 23, 7714 DOI: 10.1039/D5OB01111F

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