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Review | Special issue | Vol 99, No. 2, 2019, pp.766-813
Published online, 25th January, 2019
DOI: 10.3987/REV-18-SR(F)6
Introducing a Methyl Group into Pyridines and Quinolines: A Mini-Review

Eliezer Falb and Alfred Hassner*

*Department of Chemistry, Bar-Ilan University, Ramat-Gan 5290002, Israel


Pyridines are ubiquitous N-heterocycles that are present in many natural products and synthetic drugs with important biological applications. Introduction into a pyridine of a methyl (Me) or an isotopically labeled methyl group at carbon can alter its biological properties. However, regioselective introduction of a Me group in high yield, and preferably in a green manner, is often quite challenging. In this mini-review, several methods, most of which are recent, are examined whereby a Me or CD3 is introduced at a specific carbon in pyridines, as well as in some quinolines.