Efficient synthesis of Azabicyclo[3.1.1]heptanes via Strain-release Cycloadditions of Bicyclo[1.1.0]butanes

Abstract

Azabicyclo[3.1.1]heptanes are recognized as bioisosteres of the meta-substituted pyridine scaffold, as their bridgehead substitution mimics the arrangement of substituents on the meta-substituted pyridine. However, the synthesis of azabicyclo[3.1.1]heptanes remains underdeveloped. This mini-review highlights recent advances in their synthesis through strain-release cycloadditions of bicyclo[1.1.0]butanes.