Multiple Regioselective Functionalizations of Quinolines via Magnesiations

Abstract

A wide range of polyfunctionalized quinolines was prepared via chemo- and regioselective magnesiation reactions using appropriate Mg reagents, such as i-PrMgCl.LiCl, MesMgBr.LiCl, Mes2Mg.2LiBr, TMPMgCl.LiCl, and TMP2Mg.2LiCl. An application to the total synthesis of the biologically active compound talnetant was performed (six steps, 28%).