Housanes: Synthetic Methodologies for the Preparation of a Unique 3D Scaffold

Strained and rigid small carbocycles have gained increasing importance as synthetic tools, particularly in strain‐release reactions and as valuable bioisosteric replacements in medicinal chemistry. Among them, bicyclo[2.1.0]pentane derivatives—commonly referred to as “housanes”—have traditionally received limited attention compared to other highly strained systems, likely due to their restricted synthetic accessibility. However, recent advances in synthetic methodology have begun to reshape this landscape. This review provides an overview of the most common strategies for the construction of housanes, with particular emphasis on recent developments in the field.