Rapid production of the anaesthetic mepivacaine through continuous, portable technology

Abstract

Local anaesthetics such as mepivacaine are key molecules in the medical sector, so ensuring their supply chain is crucial for every health care system. Rapid production of mepivacaine from readily available commercial reagents and (non-dry) solvents under safe conditions using portable, continuous apparatus could make an impactful difference in underdeveloped countries. In this work, we report a continuous platform for synthesising mepivacaine, one of the most widely used anaesthetics for minor surgeries. With a focus on sustainability, reaction efficiency and seamless implementation, this platform afforded the drug in 44% isolated yield following a concomitant distillation–crystallisation on a gram scale after N-functionalisation and amide coupling, with full recovery of the solvents and excess reagents. The use of flow chemistry as an enabling tool allowed the use of “forbidden” chemistry which is typically challenging for preparative and large scale reactions in batch mode. Overall, this continuous platform presents a promising and sustainable approach that has the potential to meet the demands of the healthcare industry.