Abstract

Fluorine is Flourishing in Pharmaceuticals

Highlights

  • Since Moissan isolated elemental fluorine in 1886, fluorine has always been an element of surprise

  • The development and therapeutic monitoring of fluorinated drugs can be facilitated by additional techniques, such as 18F positron emission tomography (PET), 19F magnetic resonance imaging/spectroscopy (MRI/S) and fluorous technology, to name a few

  • There are over 150 fluorinated drugs on the market which account for about 20% of all FDA approved drugs

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Summary

Introduction

Since Moissan isolated elemental fluorine in 1886, fluorine has always been an element of surprise. In the field of pharmaceuticals, introducing a fluorine atom or fluorinated group into drugs or drug leads is often accompanied with higher binding affinity, enhanced metabolic stability, improved bioavailability, and sometimes, increased selective activity. The development and therapeutic monitoring of fluorinated drugs can be facilitated by additional techniques, such as 18F positron emission tomography (PET), 19F magnetic resonance imaging/spectroscopy (MRI/S) and fluorous technology, to name a few. With recent development in novel fluorination strategies [1,2,3,4,5,6,7,8], 18F PET, 19F MRI/S and fluorous technology [9,10,11,12], fluorine is playing an ever more important role in pharmaceuticals.

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