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.
From Lossen Transposition to Solventless "medicinal Mechanochemistry" / Porcheddu, A.; Delogu, F.; De Luca, L.; Colacino, E.. - In: ACS SUSTAINABLE CHEMISTRY & ENGINEERING. - ISSN 2168-0485. - 7:14(2019), pp. 12044-12051. [10.1021/acssuschemeng.9b00709]
From Lossen Transposition to Solventless "medicinal Mechanochemistry"
Porcheddu A.
;Delogu F.;De Luca L.;
2019-01-01
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
