Abstract: Bicyclo 1.1.1 pentane (BCP) is a kind of bridged ring skeleton with a three-dimensional structure. As a bioisostere of benzene ring, tert-butyl and alkyne, it has been widely used in the field of medicinal chemistry.With the expansion of its application, the synthesis of BCP and its derivatives has become an increasingly attractive research hotspot for scientists.Based on this, the present article summarizes the main synthetic strategies and methods of BCP derivatives, in the hope of providing some reference for drug discovery researchers and some insight for new synthetic methods of such compounds.