Organic Process Research & Development 2018-03-29

A Short Review on Synthetic Advances toward the Synthesis of Rufinamide, an Antiepileptic Drug

R. D. Padmaja, Kaushik Chanda

Index: 10.1021/acs.oprd.7b00373

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Abstract

10.1021/acs.oprd.7b00373 picture

Chronic neurological disorder of the brain is the main reason for the disease epilepsy, which affects people of almost all ages. According to World Health Organization estimates, particularly in developing regions of the world nearly 80% of people suffer from different forms of epilepsy. The majority of epileptic seizures are controlled by the use of antiepileptic drugs, which are often associated with related side effects such as blurry vision, fatigue, sleepiness, and stomach upset. Lennox–Gastaut syndrome (LGS) is childhood-onset epilepsy with multiple different types of seizures that impair intellectual development. To treat LGS, Novartis developed an antiepileptic drug known as rufinamide that contains a 1,2,3-triazole ring, and it is manufactured by Eisai under the brand name of Banzel or Inovelon. This review provides a brief background on LGS and summarizes the literature reports on different synthetic routes for rufinamide, which was approved by the U.S. Food and Drug Administration in November 2008.