Archived: Fluorine – Synthetic Methods for Selective Introduction into Small Molecule Drugs

Date: 24 April 2019

Time: 15:00 - 16:00 GMT

This FREE to attend webinar was presented by Dr John Studley, Scientific Update and was kindly sponsored by Navin Fluorine International.

The fluorine atom is now a well-established facet in the architecture of small molecule drugs. In addition to effects on a drug molecules intrinsic physiochemical properties it plays an important role in absorption and metabolism, moderates basicity of neighbouring amine functionality and, through unique stereoelectronic effects, can stabilise binding conformations for key protein interactions. This, coupled with advances in synthetic methodology and scale-up technology, has driven a year on year increase in the number of clinical candidates containing fluorine- a small number of which survive the merciless attrition statistics and become medicines.

2018 was a particularly fruitful year for the pharmaceutical industry- with 38 small molecule API’s approved by the FDA. Of these success stories, 17 (45%) contained at least one fluorine atom.

This webinar looked in detail at the synthetic methods used to selectively introduce the fluorine atom(s) into each of these molecules and explored the likely role of the element in the successful transition of these compounds from research to market.


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