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From Lossen Transposition to Solventless “Medicinal Mechanochemistry”

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journal contribution
posted on 17.06.2019, 00:00 by A. Porcheddu, F. Delogu, L. De Luca, E. Colacino
An environmentally friendly mechanochemical strategy for the preparation of unsymmetrical ureas and 3,5-disubstituted hydantoins by using safe starting materials in place of hazardous and toxic isocyanates has been designed. For the first time, the Lossen rearrangement was successfully applied to prepare a collection of relevant structures in medicinal chemistry via a one-pot mechanochemical approach and without a single drop of organic solvent including during the workup. The procedure was effective for the preparation of the Active Pharmaceutical Ingredient (API) ethotoin.