This review primarily focuses on the latest developments in Lewis acid-catalyzed strain-release cycloaddition reactions of BCBs.
A palladium-catalyzed 1,2-aminoacyloxylation of cyclopentene has been described and more structurally diverse bridged aza-bicycles could be readily achieved through further transformation.
2,5-Diazabicyclo[2.2.1]heptane (2,5-DBH) is a conformationally rigid bicyclic diamine and a privileged scaffold in medicinal chemistry, enabling diverse synthetic modifications and broad therapeutic applications across multiple disease areas.
This review summarises and highlights recent advances (year > 2015) in the medicinal chemistry applications of bridged polycyclic 3D bioisosteres of ortho-phenyl rings.
The construction of aza-3D frameworks has emerged as a pivotal strategy in drug discovery, owing to their ability to mimic heteroarene bioisosteres.