Widely used in medicinal chemistry, this compound serves as a key building block for introducing the bicyclo[1.1.1]pentane (BCP) motif into drug candidates. The BCP group acts as a bioisostere for phenyl and other aromatic rings, improving pharmacokinetic properties such as metabolic stability and solubility. It is particularly valuable in the design of peptidomimetics and CNS-targeted drugs due to its ability to enhance membrane permeability while reducing planarity. The boronic acid functionality enables facile incorporation via Suzuki-Miyaura cross-coupling, allowing rapid diversification of molecular structures during lead optimization. Its use has been reported in the development of protease inhibitors, kinase inhibitors, and other therapeutic agents where steric constraint and polarity modulation are critical.