Iridium-catalyzed C–H amidation of s-tetrazines

An efficient, selective and scalable C-H amidation of s-tetrazines under iridium(III) catalysis is reported. This reaction features a broad substrate scope, high functional group tolerance, and air and water tolerance. This reaction also shows great potential for the rapid preparation of tri- and tetra-functional building blocks, which can be applied either in bioconjugation or synthesis of DNA-encoded library.