Abstract
The authors present a mild route to a variety of aryl magnesium reagents that can be directly used in Negishi cross-coupling reactions or transmetalated for other C-C cross-couplings. Halogenated (Cl or Br) aromatics or heteroaromatics were treated with Mg(0) in the presence of LiCl at temperatures between -20 and 25 ˚C for 10 minutes to three hours. Less stable magnesium reagents like ester 5 could be transformed into their zinc derivatives 6 in situ and were further used in copper- or palladium-catalyzed reactions.
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