Direct fluorination for pharmacopoeia

Prof. G. Sandford

Prof. G. Sandford

At Durham University in England, Professor Graham Sandford has made direct fluorination in organic synthesis his specialty. Due to its very high reactivity the use of molecular fluorine in organic synthesis is a real challenge that the British team has been following for several years, thanks to elaborate synthesizing methods. The use of diluted fluorine, high dielectric constant solvents, and micro-reactors specifically designed for this purpose enables selective fluorination of a wide variety of organic molecules.

Within the framework of the European programme IMI Chem 21 (inovative medicines initiative of chemical manufacturing methods for the 21st century), the collaboration between the team of researchers at the University of Durham, the Toulouse teams of the European House of Innovative processes and the chemical engineering laboratory of ENSIACET, and the pharmaceutical company Sanofi has resulted in the conception f a continuous fluorination reactor, which allows to industrialise the synthesis by direct fluorination of a raw material allowing to obtain at a lower cost an active substance, Flucytosine.

Flucytosine, or 5-fluorocytosine, is a synthetic fluorinated analogue of cytosine, used as an antimycotic. The aim of the operation is ambitious, since it would save 650 000 African people, particularly with AIDS, the leading cause of death on this continent.



Today, the MEPI supplies up to a kg/day of raw material thanks to their micro reactor and could allow the operation to decrease by 10 of the production costs, thus making the treatment accessible to the population.