Facilitate your SAR studies by switching one of your phenyl group to the bicyclo[1.1.1]pentane. Bicyclo[1.1.1]pentane or 2-F-bicyclo[1.1.1]pentane is a phenyl isostere.
- It offers the following benefits for this isostere replacement:
- Maintain the same molecular weight
- Increase the sp3 character / reduce the flatness of the final product
- Increase solubility and permeability of the final product
- Reduce the clogp and clog D
- Increase LELP, LE (References: J. Med. Chem., 2012, 55, 3414-3424; ChemMedChem 2015, 10, 461-469)
Bellen has the intermediates and equipment (flow-photo-chemistry) to provide newer analogs upon request, from mg to kilo scale.
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