Converging Trends Brings Organic Electrochemistry To The Front Line Of Drug Discovery

The tableau was reminiscent of a Steve Jobs presentation. Phil Baran unveiled the iPad's conceptual equivalent for organic electrosynthesis. Déjà vu: the renaissance of a venerable technique, dating to the harnessed primal sparks in a tangle of wires at the hands of Faraday. It is now embodied into a sleek, standardized and almost hand-held smart reactor called the ElectraSyn 2.0, launched by IKA in close association with Baran (Refs.1,2), and well documented on YouTube for all to see in the recent ACS Fall national meeting keynote presentation: "Your Chemistry has Potential".

The significance of this development to the course of drug discovery becomes evident upon examination of the trends that converged in its development. Drug hunters have been laboring to: a) stake out new chemical real estate with more complex, 3D chemical structures via novel annulations yielding exocyclic or macrocyclic hybrid structures; b) achieve late-stage functionalization in parallel microsyntheses, including hard to implement C-H reactions; c) capitalize on microfluidic systems for continuous flow synthesis and purification, including up to kilogram scales for key fragments; and d) lower the impurity and environmental waste product burdens by resorting to heavy metal-free, greener chemistry.