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Selective Aliphatic C-H Fluorination of Molecules for Higher Potency

Direct fluorination using easily handled fluoride salts and readily prepared manganese-containing catalysts

Technology Overview

Chemists at Princeton University have discovered a powerful, simple and potentially disruptive technology for drug diversification through direct fluorination (3D-F). Fluorine is a highly desirable drug component because replacement of hydrogen with fluorine, in the case of a drug usually results in higher potency, better pharmacology, and lower metabolic burden to the patient. As a result an increasing fraction of new drug entities, as well as agrochemical compounds, contain fluorine. Another important driver for fluorinated drugs comes from PET imaging techniques that illuminate drug distributions in the body with radioactive 18F.

Major bottlenecks for the industry derive from the difficulties chemists encounter in handling toxic, corrosive and difficult to prepare fluorinating agents. This method involves easily handled fluoride

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