Abstract

Conference Opening Keynote -- Running Hazardous Chemistry in Flow – HF, F2, SF4 and More……

Oliver Kappe, Professor, Karl Franzens University of Graz

Organofluorine compounds are gaining popularity in chemical industries, especially in pharma and agrochemistry. Approximately 50% of the blockbuster drugs contain fluorine atoms. Organofluorine blockbuster drugs include e.g. atorvastatin (cardiovascular diseases), dolutegravir (HIV), emtricitabine (HIV), enzalutamide (cancer), and sitagliptin (diabetes). The introduction of fluorine atoms considerably influences the physical, chemical and biological properties of organic compounds as the bioavailability, lipophilicity or the metabolic stability of pharmaceuticals can be improved remarkably. This ever-increasing demand has transformed fluorine chemistry into a rapidly growing field of research. Despite this strong demand for fluorinated molecules in the pharma and agrochemical industry, the production of fluorinated compounds is often outsourced to specialized laboratories. This is likely the result of safety concerns in handling hazardous fluorinating reagents, alongside lack of expertise and equipment. Continuous flow chemistry has become an established method to perform hazardous reactions in a safe and controlled manner. In this lecture, contributions from our research group in the field of handling hazardous fluorinating reagents under flow conditions will be highlighted. Emphasis will be given on the safe use of HF (as amine complex), F2 (10% F2 in N2) and SF4 towards the synthesis of APIs or advanced intermediates.