Economical and Readily Accessible Preparation of o,o-Disubstituted Arylboronates through Palladium-Catalyzed Borylation of Haloarenes

Miyaura borylation, that is, palladium-catalyzed cross-coupling between bromoarenes and diboron, offers a versatile method for preparing arylboronates; however, a costly and inaccessible catalyst has been required for synthesizing highly congested arylboronates with the method. Here the Pd(OAc)(2)-tri(4-methoxyphenyl)phosphine catalyst was found to work as an efficient catalyst for the sterically demanding borylation. A broad range of o,o-disubstituted bromoarenes were converted into the corresponding arylboronates in high yields by using the palladium catalyst with Cs2CO3 in EtOAc at 80 degrees C.

Automated summary

The Miyaura borylation, using the Pd(OAc)(2)-tri(4-methoxyphenyl)phosphine catalyst, offers an efficient method for synthesizing highly congested arylboronates from o,o-disubstituted bromoarenes at 80 degrees C in EtOAc with Cs2CO3 as the base, yielding high conversion rates.