Late‐Stage Functionalisation of Pyridine‐Containing Bioactive Molecules: Recent Strategies and Perspectives

Author:

Failla Mattia1,Lombardo Giacomo W.1,Orlando Paolo1,Fiorito Daniele23ORCID,Bombonato Elena4,Ronchi Paolo5,Passarella Daniele1ORCID,Fasano Valerio1ORCID

Affiliation:

1. Department of Chemistry Università degli Studi di Milano Via Camillo Golgi, 19 20133 Milano Italy

2. School of Chemistry University of Bristol Cantock's Close, BS8 1TS Bristol UK

3. Dipartimento di Chimica, Materiali ed Ingegneria Chimica “Giulio Natta” Politecnico di Milano Piazza Leonardo da Vinci 32 20133 Milano Italy

4. Department of Chemistry “Giacomo Ciamician” Università di Bologna Via Selmi, 2 40126 Bologna Italy

5. Chemistry Research and Drug Design Chiesi Farmaceutici S.p.A Largo Belloli 11/a 43126 Parma Italy

Abstract

AbstractLate‐Stage Functionalisation (LSF) is an innovative technique that has been successfully applied to the C−H diversification of pharmaceuticals. However, LSF of the pyridine ring in drug‐like molecules is often unselective. As a result, a mixture of structurally related products is obtained, thus making the purification tedious and time‐consuming. This review shines a light on recent strategies addressing the selectivity issue in the LSF of complex natural products or drugs containing the pyridine moiety. Specifically, we have reviewed the efforts reported both in academia and industries with the hope of providing a guide for the LSF of elaborated pyridines.

Publisher

Wiley

Subject

Organic Chemistry,Physical and Theoretical Chemistry

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