Electrochemical de-aromatisation and derivatisation of fragments

Fragment Based Drug Discovery (FBDD) is a common drug discovery strategy whereby fragment libraries are screened against a target of interest. ‘Hits’ can then be grown into bigger molecules; the challenge is directional fragment growth to pick up additional interactions with the drug target. Traditionally, each new elaborated fragment requires a bespoke synthesis which can be challenging and time consuming. In the last year, new electrochemical methods have been developed. Building on the research done by the Baran group, we have developed a procedure for electrochemical fragment elaboration. The production of intermediates with nucleophilic alkenes opens up pathways that facilitate the rapid synthesis of previously inaccessible compounds.