Bicyclo[1.1.1]pentanes are novel chemical tools for bioisosteric replacement of aromatic and lipophilic groups. Bicyclo[1.1.1]pentanes are rigid scaffolds with one or two exit vectors positioned in a linear manner, thereby mimicking the para substitution pattern on arenes or tert-butyl/lipophilic moieties. Monosubstituted Bicyclo-[1.1.1]pentanes can also serve as surrogates for tert-butyl/lipophilic moieties.
For high-quality Bicyclo[1.1.1]pentanes at commercial scale, VIO Chemicals collaborates with SpiroChem, the world leader in the design and synthesis of Bicyclo[1.1.1]pentanes. SpiroChem’s novel and proprietary synthetic pathways evolve into cost -efficient manufacturing processes, which allow for largescale production of a broad range of bicyclo- [1.1.1]pentanes. In this collaboration, SpiroChem undertakes route scouting, small-scale lab synthesis and route optimisation, while VIO Chemicals performs process optimisation, technology transfer to its facilities in China and commercial scale manufacturing.
- Improved physico-chemical properties
- Improved pharmaco-kinetic properties
Bicyclo[1.1.1]pentanes are excellent chemical tools for bioisosteric replacement of aromatic groups. Due to their three-dimensional fragments, they possess equivalent or improved physico-chemical and pharmaco-kinetic properties compared to the moieties they are replacing. Especially when an arene group serves as a spacer/scaffold and it is not involved in interactions with the biological target, switching to the corresponding Bicyclo- [1.1.1]pentane is strongly advised. Bicyclo[1.1.1]- pentanes are highly recommended to medicinal chemists not only for their improved properties but also for the chemical diversity and novel IP space that they offer.
Bicyclo[1.1.1]pentanes are commonly used in drug discovery programs and the demand for these building blocks is growing exponentially.