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.We report a series of multicomponent and electrochemical approaches to perform the late-stage functionalization (MCR-LSF, e-LSF) of the 4-amino-2-pyridone chemotype under sustainable conditions.
Late-stage functionalization of the 4-amino-2-pyridone chemotype using electrochemical and MCR approaches / Giannessi, Lisa; Longo, Matteo; Massera, Chiara; Radi, Marco. - In: CHEMICAL COMMUNICATIONS. - ISSN 1359-7345. - 60:81(2024), pp. 11500-11503. [10.1039/d4cc02473g]
Late-stage functionalization of the 4-amino-2-pyridone chemotype using electrochemical and MCR approaches
Giannessi, Lisa;Longo, Matteo;Massera, Chiara;Radi, Marco
2024-01-01
Abstract
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.We report a series of multicomponent and electrochemical approaches to perform the late-stage functionalization (MCR-LSF, e-LSF) of the 4-amino-2-pyridone chemotype under sustainable conditions.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.