Rapid synthesis of 3,3′ bis-arylated BINOL derivatives using a C-H borylation in situ suzuki-miyaura coupling sequence

The increased interest in BINOL derived catalysts for asymmetric transformations has encouraged us to disclose a rapid and scalable method of preparing 3,3′ bis-arylated BINOL derivatives 1 using a one-pot CH borylation/Suzuki-Miyaura coupling sequence. The use of an aldehyde additive was found to be crucial to the success of this in situ tandem approach. This method was applied to the preparation of 10 BINOL derivatives, each completed within 24 h. Notably, this approach requires only a single purification step.