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In recent research, benzene-based aromatics have been highly disfavored in favor of aliphatic isosteric alternatives that help improve the bioavailability of organic molecules. In 2025, two groups from Janssen and Enamine reported independently innovative aromatic isosteres based on the structures of 3-oxabicyclo[3.1.1]heptane. The bicyclic molecular skeleton is highly resembling to the geometric features of the meta-substituted benzene ring, while the oxygen atom helps improve water solubility, lower lipophilicity, and increase permeability of drugs. The innovative skeleton has appeared in several patents since 2022, and this number will grow. Explore Enamine’s collection of circa 90 new building blocks containing the 3-oxabicyclo[3.1.1]heptane core skeleton.

meta-Benzene Isosteres

Concept

Concept: meta-Benzene Isosteres

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Over 50 3-oxabicyclo[3.1.1]heptanes from stock on 5-10 gram scale.

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