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Aromatic amides represent a standard and robust molecular fragment in drugs. However, their high polarity often poses a problem, reducing bioavailability. Incorporation of a fluorine atom in the vicinity of the amide enables temporary masking of the amide polarity through intramolecular hydrogen bonding, helping to improve pharmacokinetic features, especially permeability across membranes. Discover Enamines’s ortho-fluoro acids suitable for the synthesis of complex ortho-fluoroamides with improved permeability.

ortho-Fluorine for Enhances Permeability

Case study

Case study: ortho-Fluorine for Enhances Permeability

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Over 1,000 ortho-fluoro acids from stock on 5-10 gram scale.

 

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