Water-soluble non-classical benzene mimics

The concept of “Escape from the Flatland” has already gained considerable attention in medicinal chemistry. Nowadays small F(sp3)-rich structures are especially popular in drug discovery projects. In particular, replacing benzene rings with saturated bioisosteres has become an important strategy to obtain novel patent-free molecules with improved biological activity and physico-chemical profile. In this context, Enamine offers a new generation of saturated benzene mimics with improved solubility in water – 2-oxabicyclo[2.1.1]hexanes.

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more than 100 mono- and disubstituted benzene mimics with improved water solubility from stock on a 5-10 g scale:

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