Background: The canthin-4-ones are a small, yet underexplored class of natural products from
Apocynaceae plants. Efficient synthetic approaches are required for exploring this class of natural products
for drug discovery.
Objective: In this review, the synthetic approaches towards these alkaloids, as well as synthetic analogues
are summarized comprehensively. Further, the applications of canthin-4-ones as building blocks for the
synthesis of alkaloids and other polycyclic compounds of pharmaceutical interest are demonstrated.
Conclusion: Meanwhile, efficient and flexible approaches to the canthin-4-one scaffold are available
which should foster in-depth investigation of this chemotype for drug development.