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Updated: May 30, 2026

Efficient Synthesis of All-Carbon Quaternary Centers via the Conjugate Addition of Functionalized Monoorganozinc Bromides
Published on: May 26, 2019
Highly efficient one-pot access to functionalized arylboronic acids via noncryogenic bromine/magnesium exchanges
Timo Leermann1, Frédéric R Leroux, Françoise Colobert
1Laboratoire de Stéréochimie (UMR CNRS 7509), CNRS/Université de Strasbourg (ECPM), 25 Rue Becquerel, F-67087 Strasbourg, France.
A new method simplifies the synthesis of aryl boronic acids using aryl Grignard reagents. This convenient protocol achieves excellent yields at 0 °C, offering a straightforward approach for various compounds.
Area of Science:
- Organic Chemistry
- Organometallic Chemistry
Background:
- Aryl boronic acids are crucial building blocks in organic synthesis.
- Efficient methods for preparing aryl boronic acids are highly sought after.
Purpose of the Study:
- To develop a general and convenient protocol for the electrophilic borylation of aryl Grignard reagents.
- To synthesize various aryl boronic acids efficiently.
Main Methods:
- Preparation of aryl Grignard reagents from arylbromides via direct magnesium insertion (with LiCl) or Mg/Br exchange (with (i)PrMgCl·LiCl).
- Electrophilic borylation of the generated Grignard reagents.
Main Results:
- The developed protocol is general and convenient.
- Various aryl boronic acids were synthesized in excellent yields.
- The reactions proceed efficiently at 0 °C.
Conclusions:
- A straightforward and high-yielding method for synthesizing aryl boronic acids has been established.
- This protocol offers a practical approach for accessing diverse aryl boronic acids.
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