The Experts below are selected from a list of 36 Experts worldwide ranked by ideXlab platform

E. Colacino - One of the best experts on this subject based on the ideXlab platform.

  • From Lossen Transposition to Solventless “Medicinal Mechanochemistry”
    ACS Sustainable Chemistry & Engineering, 2019
    Co-Authors: A. Porcheddu, F. Delogu, L. De Luca, E. Colacino
    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.

Evelina Colacino - One of the best experts on this subject based on the ideXlab platform.

  • poly ethylene glycols and mechanochemistry for the preparation of bioactive 3 5 disubstituted hydantoins
    RSC Advances, 2016
    Co-Authors: Laure Konnert, Mouez Dimassi, Lori Gonnet, Frederic Lamaty, Jean Martinez, Evelina Colacino
    Abstract:

    Mechanochemistry was effective for the preparation of 3,5-disubstituted hydantoins from α-amino methyl esters, using either 1,1′-carbonyldiimidazole (CDI) or alkyl isocyanates. The preparation of the antimicrobial additives, 3-allyl-5,5′-dimethyl hydantoin (ADMH) and 1-chloro-3-ethyl-5,5′-dimethyl hydantoin (CEDMH) were performed by grinding. A chlorination reaction, never described before by mechanochemistry was achieved by Ca(ClO)2, while the preparation of the bioactive anticonvulsant marketed drug Ethotoin was achieved by a novel approach based on poly(ethylene) glycol (PEGs) assisted grinding.

A. Porcheddu - One of the best experts on this subject based on the ideXlab platform.

  • From Lossen Transposition to Solventless “Medicinal Mechanochemistry”
    ACS Sustainable Chemistry & Engineering, 2019
    Co-Authors: A. Porcheddu, F. Delogu, L. De Luca, E. Colacino
    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.

Laure Konnert - One of the best experts on this subject based on the ideXlab platform.

  • poly ethylene glycols and mechanochemistry for the preparation of bioactive 3 5 disubstituted hydantoins
    RSC Advances, 2016
    Co-Authors: Laure Konnert, Mouez Dimassi, Lori Gonnet, Frederic Lamaty, Jean Martinez, Evelina Colacino
    Abstract:

    Mechanochemistry was effective for the preparation of 3,5-disubstituted hydantoins from α-amino methyl esters, using either 1,1′-carbonyldiimidazole (CDI) or alkyl isocyanates. The preparation of the antimicrobial additives, 3-allyl-5,5′-dimethyl hydantoin (ADMH) and 1-chloro-3-ethyl-5,5′-dimethyl hydantoin (CEDMH) were performed by grinding. A chlorination reaction, never described before by mechanochemistry was achieved by Ca(ClO)2, while the preparation of the bioactive anticonvulsant marketed drug Ethotoin was achieved by a novel approach based on poly(ethylene) glycol (PEGs) assisted grinding.

Mi Sui Qing - One of the best experts on this subject based on the ideXlab platform.

  • Enantioselective pharmacokinetics of Ethotoin in humans following single oral doses of the racemate
    Chirality, 1992
    Co-Authors: Wayne D. Hooper, Nerida J. O'shea, Mi Sui Qing
    Abstract:

    Racemic Ethotoin (1000 mg) was administered orally as a single dose to six healthy adult volunteers. Blood samples were collected at appropriate times for 120 h following the dose. Ethotoin was quantified enantio-selectively in plasma using a novel chiral column HPLC procedure. One of the enantiomers of the chiral metabolite, 5-phenylhydantoin, was also quantified in the HPLC method. The Cmax and AUC0-infinity values for (+)-(S)-Ethotoin were significantly greater than those for (-)-(R)-Ethotoin (ratio of mean AUC0-infinity values 0.88), but the elimination half-lives of the isomers were virtually identical [12.35 +/- 5.15 h for (-)-(R)-Ethotoin; 12.28 +/- 5.34 h for (+)-(S)-Ethotoin]. Parameters derived from AUC0-infinity (Cl0/F and V(area)/F) also differed slightly between the isomers. The data were interpreted as indicating a small difference in the absorption of the two isomers; it seemed unlikely, in terms of the identical elimination rates, that their metabolic profiles would differ greatly. The 5-phenylhydantoin was eliminated with a significantly longer half-life (18.69 +/- 6.11 h) than that of Ethotoin. Enantioselectivity in the pharmacokinetics of Ethotoin is therefore a minor issue.