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Double Cu‐Catalyzed Direct Csp3−H Azidation/CuAAC Reaction: A Direct Approach towards Demanding Triazole Conjugates

Brandhofer, Tobias ; Özdemir, Aysegül ; Gini, Andrea ; Mancheño, Olga García


The first one-pot procedure for the double copper(I)-catalyzed oxidative Csp(3)-H azidation-CuAAC process, implying unstable azide intermediates and easy-to-remove reagents under water-tolerant conditions, is presented. The combination of tert-butyl hydroperoxide as oxidant and TMSN3 as azide source for the C-H bond azidation, which produces harmless side-products such as tBuOH and H2O, probed to ...


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