Organic Letters· 2026Q1
Ruthenium-Catalyzed Site-Selective Direct Deuteration of Azaarenes Using Deuterium Oxide
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- 2026year
Short summary
A ruthenium complex, [{(η6-p-cymene)RuCl}2(μ-H-μ-Cl)], enables site-selective deuteration of C–H bonds in five-membered azaarenes using D2O as the deuterium source, with minimal catalyst loading (0.5–1 mol%).
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Key points
- Ruthenium complex [{(η6-p-cymene)RuCl}2(μ-H-μ-Cl)] catalyzes site-selective deuteration of C–H bonds in five-membered azaarenes.
- D2O is used as a direct deuterium source, achieving good to excellent deuterium incorporation in imidazole, thiazole, and indole derivatives.
- The reaction requires minimal catalyst loading (0.5–1 mol%).
- Active drug substances can be directly deuterated under these conditions.
AI-generated from the title and abstract; the full text is not read.
Abstract
Abstract Selective incorporation of deuterium into heteroarenes without directing groups has been a long-standing problem. Monohydrido-bridged ruthenium complex [{(η6-p-cymene)RuCl}2(μ-H-μ-Cl)] catalyzes the site-selective deuteration of C–H bonds in five-membered azaarenes. Notably, active drug substances were directly deuterated under this catalytic condition. Remarkably, the reaction requires a minimal catalyst loading (0.5–1 mol %) and D2O is employed as a direct deuterium source for the deuteration of imidazole, thiazole, and indole derivatives that exhibited good to excellent deuterium incorporation.
The authors' abstract, as published at the source. Organic Letters, 2026 · DOI ↗
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Field: Pharmaceutical Science
Pharmaceutical SciencePharmacology, Toxicology and Pharmaceutics