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Review | Regular issue | Vol 91, No. 3, 2015, pp.479-504
Published online, 6th February, 2015
DOI: 10.3987/REV-14-816
Directed Lithiation and Substitution of Pyridine Derivatives

Gamal A. El-Hiti,* Keith Smith,* and Amany S. Hegazy

*Department of Optometry, College of Applied Medical Sciences, King Saud University, P.O. Box 10219, Riyadh 11433, Saudi Arabia

Abstract

Directed lithiation of substituted pyridines containing a directing metalating group (DMG) with a lithium reagent in anhydrous solvent at low temperature gives the corresponding lithium intermediates in-situ, which on reactions with electrophiles produce the corresponding substituted derivatives. The method is simple, general, convenient and often high yielding.