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Article Dans Une Revue ACS Sustainable Chemistry & Engineering Année : 2019

From Lossen Transposition to Solventless “Medicinal Mechanochemistry”

Résumé

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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Dates et versions

hal-02280126 , version 1 (06-09-2019)

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Citer

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