Used as a key building block in medicinal chemistry for the synthesis of strained bioisosteres, particularly in the development of novel drug candidates. Its unique bridgehead structure enables improved pharmacokinetic properties when incorporated into molecules, such as enhanced metabolic stability and altered lipophilicity. Commonly employed in fragment-based drug design and in the preparation of bicyclo[1.1.1]pentane derivatives that serve as replacements for phenyl or tert-butyl groups. Also utilized in late-stage functionalization through cross-coupling reactions due to the presence of the iodine atom, allowing for efficient diversification in compound libraries.