Mild Condition Synthesis of Quinoxaline Derivatives

The quinoxaline scaffold, comprising a fused benzene and pyrazine ring, underpins a wealth of bioactive and functional materials. Traditionally, quinoxaline derivatives have been prepared via high-temperature condensations or harsh oxidative cyclisations, often requiring strong acids or metal reagents. In contrast, mild condition approaches now enable assembly and functionalisation under ambient temperature, neutral pH or in aqueous media, frequently exploiting light, benign oxidants or biocatalysts. These methods reduce energy input, minimise by-products and expand the scope of substituents—particularly fluorinated groups and chiral centres—without compromising yield or selectivity. Such advances support greener manufacture of pharmaceuticals, agrochemicals and optoelectronic materials, and facilitate late-stage diversification of complex molecules. Cross-disciplinary strategies—combining photoredox catalysis, decarboxylative couplings, multicomponent reactions and chemoenzymatic sequences—have converged to deliver quinoxaline derivatives with improved functional complexity and enantioselectivity under remarkably mild conditions.

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Mild Condition Synthesis of Quinoxaline Derivatives publication trend

The graph below shows the total number of articles in mild condition synthesis of quinoxaline derivatives across all publications each year (not limited to Nature Index journals).

Technical terms

Photoredox catalysis: Use of light-activated catalysts to drive redox reactions via radical intermediates under mild conditions.

Decarboxylative coupling: Formation of C–C bonds through removal of carbon dioxide from carboxylate precursors, often under gentle heating or irradiation.

Chemoenzymatic synthesis: Integration of chemical and enzymatic steps to construct complex molecules with high stereocontrol at ambient temperature.

References

1. Photoinitiated decarboxylative C3-difluoroarylmethylation of quinoxalin-2(1 H )-ones with potassium 2,2-difluoro-2-arylacetates in water. RSC Advances (2020).
2. Radical Addition of Dihydroquinoxalin-2-ones to Trifluoromethyl Ketones under Visible-Light Photoredox Catalysis. The Journal of Organic Chemistry (2022).
3. Chemoenzymatic Asymmetric Synthesis of Complex Heterocycles: Dihydrobenzoxazinones and Dihydroquinoxalinones. ACS Catalysis (2022).