The benzene ring is the most common structural fragment in drugs. In 2019, two groups, one from Enamine and another from Merck, independently introduced difluorobicyclo[1.1.1]pentane, a structure that matches the exact molecular volume of benzene. The isosteric replacement of a phenyl ring with difluorobicyclo[1.1.1]pentane maintains the molecular volume while substantially increasing the sp³-character and elevating the solubility of the molecule. Since 2019, our chemists have expanded the panel of difluorobicyclo[1.1.1]pentanes for use in medicinal chemistry.
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Over 50 difluorobicyclo[1.1.1]pentanes from stock on 5-10 gram scale.
