Selective Alkylation of Complex Molecules in Flow

ended

"Developing new pharmaceutically-active molecules for the treatment of diseases that compromise the health and well-being of society is an essential but tedious process with rising costs, partially due to the arduous chemical synthesis of complex drug candidates. Recently, innovations in organic chemistry have streamlined the access to vast libraries of drugs by applying novel methodologies such as Late-Stage Functionalization of C-H bonds. However, one of the major challenges of editing biologically-active chemical structures is the development of processes that are compatible with diverse functional groups and functionalize one single position ""à la carte"" in an efficient and predictable manner. SELECTFLOW presents a multidisciplinary project that lies in the intersection of synthetic photoredox catalysis with microfluidic technologies, with the objective of delivering a selective, sustainable and predictable methodology for the modification of biologically-active molecules using light alkanes as raw materials. This will require the accomplishment of three specific objectives: 1) Development of a chemo- and regioselective synthetic methodology for the edition of nitrogen-containing aromatic heterocycles. 2) Translation of the developed photocatalytic system into a microflow-based setup, to enable the use of gaseous reagents in a milder and scalable fashion. 3) Understanding the mechanistic intricacies of the developed methodology in order to predict unexplored similar transformations. Overall, this proposal directly tackles one of the most important challenges for the pharmaceutical industry, the rapid and cost-effective production of innovative drugs, by delivering a sustainable valorisation of greenhouse gases, such as methane. It is expected that this innovative approach will be of high scientific, technological and societal impact, ultimately reinforcing the already European competitiveness in the production of life-saving drugs."