Highly Efficient Magnesiation of Functionalized Arenes and Heteroarenes

Significance

The direct selective metallation of arenes and hetarenes is an extremely synthetically attractive process, which allows an easy polyfunctionalization of these compounds. Such metallation usually requires cryogenic temperatures and/or large excess of a base. This new method has many excellent advantages: only a slight excess of the metallating reagent is required, the reactions are almost always chemoselective and proceed at temperatures usually not below -30 °C. The reactions of the resulting organometallic species with electrophiles uniformly give excellent yields of products.