A novel synthetic approach for the orphan drug Levetiracetam

Levetiracetam is an orphan drug used to treat epilepsy in newborns. Since 2010, it is part of the list of the best drugs sold and many efforts are done for the development of newer and more efficient synthesis, providing this attractive bioactive molecule. We report the development of a new synthetic approach that combines organophotocatalysis with the chemistry of nitrogen radicals to access an advanced known intermediate of Levetiracetam (Figure 1).2,3 A few further steps allow to access the drug in good overall yield and moderate enantiometic excess. The development of a telescoped process under flow conditions is object of study in our research group, and it represents an appealing alternative to the established routes, also on the big scale.