C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 315/06 (2006.01) C07C 315/02 (2006.01) A61K 31/16 (2006.01) C07C 317/44 (2006.01)
Patent
CA 2511992
The present invention is directed to an improved process for preparing modafinil wherein benzhydrylthioacetamide is prepared in high yield and purity by the reaction of a haloacetamide with the reaction product of thiourea and benzhydrol in aqueous solution. The reaction employing the haloacetamide is conducted in a solvent comprising water and an organic solvent such as dimethylformamide having dissolved therein a basic salt such as potassium carbonate. The resulting benzhydrylthioacetamide can be oxidized to provide the pharmaceutical modafinil.
La présente invention a trait à un procédé amélioré pour la préparation de modafinile dans lequel on prépare du benzhydrylthioacétamide à grand rendement et pureté élevée par la réaction d'un haloacétamide avec le produit réactionnel de thiourée et benzhydrol en solution aqueuse. La réaction à l'aide d'haloacétamide est effectuée dans un solvant comprenant de l'eau et un solvant organique tel que du diméthylformamide comportant en solution un sel de base tel que le carbonate de potassium. Le benzhydrylthioacétamide obtenu peut être oxydé pour fournir du modafinile pharmaceutique
Mallinckrodt Inc.
Osler Hoskin & Harcourt Llp
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