Oxidation method for preparing highly pure modafinil,...

Single-crystal – oriented-crystal – and epitaxy growth processes; – Processes of growth from liquid or supercritical state – Having growth from a solution comprising a solvent which is...

Reexamination Certificate

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C117S069000, C117S937000, C117S939000, C424S451000, C424S464000, C514S618000

Reexamination Certificate

active

06849120

ABSTRACT:
The present invention provides an improved process for preparing modafinil, whereby it may be isolated in high purity by a single crystallization. The process produces modafinil free of sulphone products of over-oxidation and other byproducts. The invention further provides new crystalline Forms II-VI of modafinil and processes for preparing them. Each of the new forms is differentiated by a unique powder X-ray diffraction pattern. The invention further provides pharmaceutical compositions containing novel modafinil Forms II-IV and VI.

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Josef Drabowicz et al. “A Convenient Procedure for the Oxidation of Sterically Hindered Sulfides to Sulfoxides” Synthesis—Journal of Synthetic Organic Chemistry—Oct. 1990.
Jerry March “Reactions, Mechanisms, and Structure” Advanced Organic Chemistry, Fourth Edition.
Th. Becue et al. “Confirmation of the Structure of by-products in the synthesis of Modafinil by liquid chromatography-mass spectrometry” Journal of Chromatography, 557 (1991) 489-494.
Renault J. Guillon et al “Synthesis and CNS Activity of New 3-Amino-3-arylpropionic Acid Derivatives”, Pharm. Pharmacol. Commun. 1999, 5:217-223.

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