The first general protocol for <i>N</i>-monoalkylation of sulfamate esters: benign synthesis of <i>N</i>-alkyl Topiramate (anticonvulsant drug) derivatives

A novel protocol for the highly selective <i>N</i>-monoalkylation of the sulfamate ester moiety has been developed. This reaction proceeded efficiently using alkyl halides, benzyl halides and α-halo ketones as the electrophile in the presence of KF-Al₂O₃ as a cost-effective and robust catalyst. This approach provides new access to <i>N</i>-monoalkylated Topiramate (anticonvulsant drug) derivatives which are potentially of great importance in medicinal chemistry.