Rhodaelectro-catalyzed C–H activations directed by pharmacophores: enabling modification of bioactive compounds†

In the realm of sustainable molecular synthesis, metallaelectro-catalysis has emerged as a highly potent platform over the past decade. While significant advancements have been achieved in this field, the development of strategies for late-stage C–H functionalization remains a formidable challenge. In this context, we present an electrochemical rhodium-catalyzed C–H activation strategy that facilitates the selective modification of bioactive compounds. The developed electrocatalysis strategy, enabling the efficient C–H/N–H activations and annulations with a variety of diaryl-, dialkyl-, and unsymmetric alkynes, demonstrates broad tolerance towards a range of medicinally relevant functional groups and thus provides expedient access to the modification of bioactive compounds.