Scope of the Two-Step,
One-Pot Palladium-Catalyzed Borylation/Suzuki Cross-Coupling Reaction
Utilizing Bis-Boronic Acid
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Abstract
The use of bis-boronic acid for the direct synthesis
of boronic acids has greatly facilitated the two-step, one-pot borylation/Suzuki
cross-coupling reaction between aryl and heteroaryl halides. With
use of Buchwald’s second-generation XPhos preformed catalyst,
high yields of cross-coupled products were obtained for most substrates.
The method also allows an efficient two-step, one-pot synthesis, providing
access to three distinct cross-coupled products after column chromatography.
The method also provides a rapid and convenient route to teraryl compounds
