Recent Advances in the Synthesis of Bicyclo[3.1.1]heptanes

In the past three years, bicyclo[3.1.1]heptanes and their structural analogues have emerged as useful bioisosteres of meta-substituted (hetero)arenes. To meet increasing demand for bicyclo[3.1.1]heptanes, chemists have developed a plethora of novel methods for their synthesis. In this review, we assess research progress on their synthesis and functionalization, considering both scope and mechanism. In addition, we discuss the challenges posed by and outlook for the identification of novel reaction manifolds to access novel functionalized bicyclo[3.1.1]heptanes.