We have developed a novel strategy from simple and readily available substrates for the synthesis of N-1 substituted hydantoin, thiohydantoin and iminohydantoin under solvent-free reaction conditions. The products were obtained in quantitative yields with high purity. Syntheses of wide varieties of hydantoin, thiohydantoin and iminohydantoin bearing primary, secondary, tertiary cyclic and aryl groups were successfully achieved, and product isolation was very straightforward. Convenient syntheses of bicyclohydantoins and bis-hydantoins are one of the most striking features of this reaction. Our approach may be useful to chemists seeking novel synthetic fragments with unique properties for medicinal chemistry programs.

Novel, efficient and greener protocol for the syntheses of hydantoin, thiohydantoin and iminohydantoin from common precursor

243rd National Meeting (2012)

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