BIOISOSTERES compounds!

Phenyl
Isotere

BIOISOSTERES compounds!

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.
Ask for more: full list in sdf, custom synthesis, quote.
sales.europe@bellenchem.eu