Facile One-Pot Synthesis of Substituted Hydantoins from Carbamates

    August 2017 in “Synlett
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    TLDR Scientists in India found a safer and efficient way to make a type of medicine called hydantoins from carbamates, which also worked well in making the seizure medicine, Ethotoin.
    In 2017, researchers from the National Institute of Pharmaceutical Education and Research in India developed a simple and efficient method for synthesizing 3-substituted, 5-substituted, or 3,5-disubstituted hydantoins from carbamates. The process involved reacting a-amino methyl ester hydrochlorides with carbamates to produce ureido derivatives, which then cyclized under basic conditions to yield substituted hydantoins. This method was used to synthesize the anticonvulsant drug ethotoin, avoiding the use of hazardous reagents typically used in such syntheses. The procedure had a broad substrate scope and consistently produced good to excellent yields under mild conditions. The method was also applied in a gram-scale synthesis of Ethotoin, yielding a 78% success rate.
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