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Preparation of 6-aminocyclohepta-2,4-dien-1-one Derivatives via Tricarbonyltroponeiron
Published on: August 12, 2019
Late-stage functionalization of the 4-amino-2-pyridone chemotype using electrochemical and MCR approaches
Lisa Giannessi1, Matteo Longo1, Chiara Massera2
1Dipartimento di Scienze degli Alimenti e del Farmaco (DipALIFAR), Università degli Studi di Parma, Viale delle Scienze, 27/A, 43124 Parma, Italy. marco.radi@unipr.it.
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.
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