A New CuI/Oxalamide Catalytic System for the Large‐Scale Aerobic Oxidation of Alcohols

Since the report of oxamide ligands, they have been widely used for the efficient construction of various types of C−X (such as C, N, O and S) bonds. To evaluate whether the easily tunable electronic properties and unique coordination modes of oxamide ligands can also shine in the field of oxidation, we initiated a study on oxamide ligand/copper/air oxidation and applied it to the oxidation of alcohols to assess its practicality and potential applications. The practicality of this strategy was further verified through scale‐up reactions on a 100 mmol scale and gram‐scale derivatization of pharmaceutical molecules. The initial example illustrates the remarkable catalytic oxidation capacity of oxalamide/CuI in the oxidative field and its prospective applications. It demonstrates mild oxidizing power at room temperature under air (Example 53), with excellent selectivity towards primary alcohols and completed 100 mmol scale‐up. In addition, the structural modification of bioactive molecule derivatives and the derivatization of drug molecules have also been successfully achieved.