The article discusses the importance of developing new synthetic methodologies for drug discovery, particularly focusing on saturated arene bioisosteres. The authors present a novel method to synthesize the bicyclo[2.1.1]hexane scaffold using mild conditions and a straightforward protocol. This synthesis involves coupling cyclic allenes and bicyclo[1.1.0]butanes, both of which have significant strain energies. The reaction proceeds via a diradical pathway driven by the intrinsic diradical character of the reactants, suggesting new avenues for exploration in chemical synthesis and drug development.
The incorporation of bioisosteres typically leads to favorable drug-like properties and represents an emerging field of research.
Our studies provide a means to access functionalized bicyclo[2.1.1]hexanes of value for drug discovery.
Reactivity arises from innate diradical character present in each reactant, stemming from severe geometric distortions.
This methodology enables uncommon modes of reactivity and encourages the strategic use of diradicaloids in chemical synthesis.
Collection
[
|
...
]