Abstract
AbstractWell‐defined ruthenium(II) biscarboxylate complexes enabled selective ortho‐deuteration with weakly‐coordinating, synthetically useful carboxylic acid with outstanding levels of isotopic labeling. The robust nature of the catalytic system was reflected by a broad functional group tolerance in an operationally‐simple manner, allowing the isotope labeling of challenging pharmaceuticals and bioactive heterocyclic motifs. The synthetic power of our method was highlighted by the selective tritium‐labeling of repaglinide, an antidiabetic drug, providing access to defined tritium labeled therapeutics.
Highlights
C H moieties of pharmaceuticals are still one of the key challenges,[5] because the catalyst needs to be compatible with a variety of functional groups that are commonly present in marketed pharmaceuticals
MacMillan described the direct Hydrogen isotope exchange (HIE) of α-amino C H bonds mediated by photoredox catalysis (Figure 1b).[11]
Hydrogen isotope exchange (HIE) of otherwise inert C H bonds promoted by transition-metal catalysts has emerged as a valuable tool for the clarification of reaction mechanisms, as reference materials in mass-dependent analytical chemistry and for the improvement of bioactive drugs in pharmaceutical industries.[1]
Summary
C H moieties of pharmaceuticals are still one of the key challenges,[5] because the catalyst needs to be compatible with a variety of functional groups that are commonly present in marketed pharmaceuticals. Activation of organic molecules,[9] selective HIE of pharmaceuticals continuous to be extremely rare. Well-defined ruthenium(II) biscarboxylate complexes enabled selective ortho-deuteration with weakly-coordinating, synthetically useful carboxylic acid with outstanding levels of isotopic labeling.
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