Antiepileptic Drug Rufinamide: Synthesis and Process Impurities

Abstract

This paper presents an efficient and practical protocol for the synthesis of rufinamide (anti-epileptic drugs) active pharmaceutical ingredient (API) and several process impurities by a 1,3-dipolar cycloaddition reaction, starting from commercially available benzyl bromides. The earlier reported syntheses of rufinamide had encountered challenges in isolating by-products from the mother liquor. In this work, the impurities were synthesized via the retrosynthesis route to serve as reference samples for assessing the purity level of drugs. These impurities, characterized by the presence of N-group and azole derivatives, find wide-range applications in academic and industrial settings, including organic synthesis, drug discovery, polymer chemistry, chemical biology, and supramolecular chemistry. The primary objective of this synthesis was to propose a reliable and pragmatic method for producing rufinamide and its impurities to address diverse scientific and industrial requirements. The protocol outlined in this research aims to contribute to the development of robust methodologies for the synthesis of pharmaceuticals and associated impurities, with potential implications for drug development and chemical research.