Recent advances in the preparation of active pharmaceutical ingredient (S)-Pregabalin

In recent times, several efforts have been devoted to develop new synthetic methodologies to access active the pharmaceutical ingredient (S)-Pregabalin. Marketed as (LyricaTM), (S)-Pregabalin is indicated for the treatment of epilepsy, neuropatic pain and anxiety. As presented in this short review, the methodologies available to prepare (S)-Pregabalin can be classified by the method employed to install the desired absolute stereochemistry, namely: (a) preparation of Pregabalin as a racemate and its resolution; (b) enantioselective syntheses; (c) processes involving a biocatalytic step. This review provides an overview of the state of the art on the synthetic methodology available to prepare this blockbuster API.