C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 323/52 (2006.01) C07C 317/44 (2006.01)
Patent
CA 2543326
The present invention is directed to an improved process for preparing modafinil wherein benzhydrylthioacetate is prepared in high yield and purity by the reaction of a haloacetate with the reaction product of thiourea and benzhydrol. The reaction employing the haloacetate is conducted in a solvent comprising an organic solvent such as methanol having dissolved therein an organic base or an inorganic basic salt such as sodium bicarbonate. The resulting benzhydrylthioacetate can be amidated and then oxidized to provide the pharmaceutical grade modafinil in high yield and purity.
L'invention concerne un procédé amélioré permettant de préparer un modafinil dans lequel un benzhydrylthioacétate à rendement et pureté élevés est préparé par réaction d'un haloacétate avec le produit de réaction de thiourée et de benzhydrol. La réaction utilisant l'haloacétate est effectuée dans un solvant comprenant un solvant organique, tel qu'un méthanol dans lequel une base organique ou un sel basique inorganique tel qu'un bicarbonate de sodium, est dissous. Le benzhydrylthioacétate résultant peut être amidé, puis oxydé afin de produire un modafinil de qualité pharmaceutique à rendement et à pureté élevés.
Mallinckrodt Inc.
Mallinckrodt Llc
Osler Hoskin & Harcourt Llp
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