We describe a palladium-catalyzed
nondirected late-stage deuteration
of arenes. Key aspects include the use of D2O as a convenient
and easily available deuterium source and the discovery of highly
active N,N-bidentate ligands containing an N-acylsulfonamide
group. The reported protocol enables high degrees of deuterium incorporation
via a reversible C–H activation step and features extraordinary
functional group tolerance, allowing for the deuteration of complex
substrates. This is exemplified by the late-stage isotopic labeling
of various pharmaceutically relevant motifs and related scaffolds.
We expect that this method, among other applications, will prove useful
as a tool in drug development processes and for mechanistic studies.
We describe a palladium catalyzed non-directed late-stage deuteration of arenes. Key aspects include the use of D2O as a convenient and easily available deuterium source and the discovery of highly active N,N-bidentate ligands containing an N-acyl sulfonamide group. The reported protocol enables high degrees of deuterium incorporation via a reversible C-H activation step and features an extraordinary functional group tolerance, allowing for the deuteration of complex substrates. This is exemplified by the late-stage isotopic labelling of various pharmaceutically relevant motifs and related scaffolds. We expect that this method, amongst other applications, will prove useful as a tool in drug development processes and for mechanistic studies.
The synthesis and coordination chemistry of Rh(i) complexes bearing a tris(isopropyl)-azaphosphatrane (TiPrAP) ligand are reported. The adaptive nature of TiPrAP ligands allows for molecular control of the immediate environment of the metal center.
We describe a palladium catalyzed non-directed late-stage deuteration of arenes. Key aspects include the use of D2O as a convenient and easily available deuterium source and the discovery of highly active N,N-bidentate ligands containing an N-acyl sulfonamide group. The reported protocol enables high degrees of deuterium incorporation via a reversible C-H activation step and features an extraordinary functional group tolerance, allowing for the deuteration of complex substrates. This is exemplified by the late-stage isotopic labelling of various pharmaceutically relevant motifs and related scaffolds. We expect that this method, amongst other applications, will prove useful as a tool in drug development processes and for mechanistic studies.
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