61764-82-7Relevant articles and documents
Palladium-Catalyzed Nondirected Late-Stage C-H Deuteration of Arenes
Farizyan, Mirxan,Mondal, Arup,Mal, Sourjya,Deufel, Fritz,Van Gemmeren, Manuel
supporting information, p. 16370 - 16376 (2021/10/21)
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.