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Highly Efficient One-Pot Access to Functionalized Arylboronic Acids via Noncryogenic Bromine/Magnesium Exchanges

Timo Leermann, Frédéric R. Leroux* and Françoise Colobert*

*Laboratoire de Stéréochimie (UMR CNRS 7509), CNRS/Université de Strasbourg (ECPM), 25 Rue Becquerel, F-67087 Strasbourg, France, Email:,

T. Leermann, F. R. Leroux, F. Colobert, Org. Lett., 2011, 13, 4479-4481.

DOI: 10.1021/ol2016252 (free Supporting Information)

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A general and convenient protocol for the electrophilic borylation of aryl Grignard reagents prepared from arylbromides by direct insertion of magnesium in the presence of LiCl or by Mg/Br exchange with iPrMgCl·LiCl enables the synthesis of various aryl boronic acids in a straightforward manner in excellent yields at 0°C.

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Key Words

arylboronic acids

ID: J54-Y2011-2380