From Lossen Transposition to Solventless “Medicinal Mechanochemistry”

Abstract : 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.
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https://hal.umontpellier.fr/hal-02280126
Contributeur : Odile Hennaut <>
Soumis le : vendredi 6 septembre 2019 - 09:20:55
Dernière modification le : mercredi 9 octobre 2019 - 12:54:02

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A. Porcheddu, F. Delogu, L. de Luca, E. Colacino. From Lossen Transposition to Solventless “Medicinal Mechanochemistry”. ACS Sustainable Chemistry & Engineering, American Chemical Society, 2019, 7 (14), pp.12044-12051. ⟨10.1021/acssuschemeng.9b00709⟩. ⟨hal-02280126⟩

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