化学
钯
氘
催化作用
齿合度
组合化学
功能群
药物发现
立体化学
计算化学
金属
有机化学
生物化学
量子力学
物理
聚合物
作者
Mirxan Farizyan,Arup Mondal,Sourjya Mal,Fritz Deufel,Manuel van Gemmeren
摘要
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.
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