Late-stage functionalization of the 4-amino-2-pyridone chemotype using electrochemical and MCR approaches.

We report the development and application of different strategies for the late-stage functionalization (LSF) of the biologically relevant 4-amino-2-pyridone chemotype. Using the recently discovered PCSK9 inhibitor 5c as a prototype, a series of electrochemical LSF (e-LSF) and multicomponent LSF (MCR-LSF) have been set-up to decorate the 4-amino-2-pyridone scaffold. The usefulness of these methods has been demonstrated by generating a series of novel derivatives in a site-selective and sustainable way.