Synthetic Routes to Approved Drugs Containing a Spirocycle

The use of spirocycles in drug discovery and medicinal chemistry has been booming in the last two decades. This has clearly translated into the landscape of approved drugs. Among two dozen clinically used medicines containing a spirocycle, 50% have been approved in the 21st century. The present review focuses on the notable synthetic routes to such drugs invented in industry and academia, and is intended to serve as a useful reference source of synthetic as well as general drug information for researchers engaging in the design of new spirocyclic scaffolds for medicinal use or embarking upon analog syntheses inspired by the existing approved drugs.

Automated summary

The use of spirocycles in drug discovery and medicinal chemistry has seen significant growth in the past two decades, with 50% of clinically used medicines containing a spirocycle being approved in the 21st century. This review focuses on synthetic routes to such drugs developed in industry and academia, serving as a valuable reference for researchers in the design of new spirocyclic scaffolds or analog syntheses inspired by approved drugs.