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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.

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A highly efficient, clean, and simple procedure for the synthesis of a privilege imidazo[4,5- b ]pyridine scaffold from 2-chloro-3-nitropyridine in combination with environmentally benign H 2 O-IPA as a green solvent is presented. The scope of the novel method has been demonstrated through the tandem sequence of S N Ar reaction with substituted primary amines followed by the in situ nitro group reduction and subsequent heteroannulation with substituted aromatic aldehydes to obtain functionalized imidazo[4,5- b ]pyridines with only one chromatographic purification step. The synthesis pathway appears to be green, simple, and superior compared with other already reported procedures, with the high abundance of reagents and great ability in expanding the structural diversity.

The one-pot telescopic approach has been developed for the chemoselective synthesis of substituted benzo­[e]­pyrido/pyrazino/pyridazino­[1,2-b]­[1,2,4]­thiadiazine dioxides using readily available 2-aminopyridines/pyrazines/pyridazine and 2-chloro benzene sulfonyl chloride. This one-pot procedure involves the chemoselective sulfonylation of 2-aminopyridines/pyrazines/pyridazine with 2-chloro benzene sulfonyl chloride followed by a Cu­(I)-catalyzed Ullmann-type C–N coupling reaction to obtain benzo­[e]­pyrido/pyrazino/pyridazino­[1,2-b]­[1,2,4]­thiadiazine dioxides with broad substrate scope and high functional group tolerance. The synthetic sequence merges well with the nucleophilic attack on the 2-amino group of pyridines/pyrazines/pyridazines on the 2-chloro benzene sulfonyl chloride, followed by Cu­(I)-catalyzed ipso chloro displacement to C–N bond formation resulting in a more modular and straightforward approach. Moreover, the biological significance of the synthesized benzothiadiazine dioxides was evaluated by following their ability to bind to protein macromolecules and their anti-inflammatory activity.