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This Minireview focuses on selected topics in the syntheses of bicyclo[1.1.1]pentane (BCP) analogues. A brief historical introduction was included. The content covers various synthetic routes of 1‐substituted and 1,3‐disubstituted BCPs. Selective examples of synthetically useful building blocks are summarized for each category for synthetic organic chemists' and medicinal chemists' reference. A compare‐and‐contrast analysis is also applied to evaluate these routes and to demonstrate the progress of strategic functional group transformations using modern organic methodologies. By systematically analyzing the synthetic strategies to access these strained molecules, we also hope that this Minireview will provide inspirations for future developments in this area. [ABSTRACT FROM AUTHOR]