Copper-Mediated and Copper-Catalyzed Cross-Coupling of Indoles and 1,3-Azoles: Double CH Activation

A new bronze age: The described copper‐mediated cross‐coupling with double CH activation can provide a convergent access to indole‐containing biheteroaryls that are of high interest in pharmaceutical and medicinal chemistry. In this strategy an easily attachable and detachable 2‐pyrimidyl directing group is used. Moreover, a variant that is catalytic in copper is achieved by using atmospheric oxygen as an ideal co‐oxidant (see scheme).