Abstract
Dibenzoxepines have gained privileged status in medicinal chemistry and drug discovery
due to their appearance in various natural products and life-saving drug molecules.
Dibenzoxepine-based molecules, such as artocarpols, asenapine, and pacharin, possess
a wide range of biological activities including anti-inflammatory, antidepressant,
antihypertensive, antiestrogenic, and insecticidal activities. Therefore, designing
and developing new methodologies to access the dibenzoxepine core has become a paramount
research topic for organic/ medicinal chemists. Herein, we reviewed various synthetic
methods to access dibenzoxepine derivatives. The total syntheses of dibenzoxepine-based
natural products and biologically/medicinally important molecules have also been reviewed.
1 Introduction
2 Transition-Metal-Free Approaches
2.1 Acid-Mediated Transformations
2.2 Base-Mediated Transformations
2.3 NHC-Organocatalyzed Transformations
2.4 Miscellaneous
3 Metal-Mediated Approaches
4 Transition-Metal-Catalyzed Approaches
4.1 Iron-Catalyzed Transformations
4.2 Copper-Catalyzed Transformations
4.3 Ruthenium-Catalyzed Transformations
4.4 Palladium-Catalyzed Transformations
4.5 Other Transition-Metal-Catalyzed Transformations
5 Total Syntheses
6 Conclusion
Key words
dibenzoxepine - NHC organocatalysis - transition-metal catalysis - S
NAr reaction - natural products - active pharmaceutical ingredients (APIs)
