Scott Perrin - Boothwyn PA, US Kimm Galbraith - Spring City PA, US Naidong Ye - Malvern PA, US
Assignee:
Vela Pharmaceuticals, Inc. - Ewing NJ
International Classification:
A61K031/5513 C07D243/00
US Classification:
514/221000, 540/567000
Abstract:
(R)-tofisopam, substantially free of the (S)-enantiomer of tofisopam, is obtained by separating the enantiomers of tofisopam by chromatography employing a chiral separation medium comprising (i) (2S)-2-{(1S)[(3,5-dinitrophenyl)carbonylamino]phenylmethyl}-3,3-dimethylbutanoate, covalently bound to silica through an alkylene ester linkage or (ii) an amylose derivative of formula I: wherein each Rand n are defined herein; the amylose derivative being coated on a porous inorganic carrier or a porous organic carrier.
Scott Perrin - Boothwyn PA, US Naidong Ye - Malvern PA, US Kimm Galbraith - Spring City PA, US Wilhelm Hauck - Wallingford PA, US
Assignee:
Vela Pharmaceuticals, Inc. - Ewing NJ
International Classification:
C07D 243/10
US Classification:
540567000
Abstract:
The present invention is directed to a process for the isolation of (R)-tofisopam with high enantiomeric purity and high overall yields from a mixture of tofisopam enantiomers by means of a non-steady state continuous chromatographic process.
Conversion Process For 2,3-Benzodiazepine Enantiomers
Yong Wei - Branchburg NJ, US Naidong Ye - Malvern PA, US Kimm Galbraith - Spring City PA, US Jianfeng Shi - Baltimore MD, US Wuyi Wang - Silver Spring MD, US Yungen Xu - Baltimore MD, US Mallikarjun Ravi - Baltimore MD, US
Assignee:
Vela Pharmaceuticals, Inc. - Ewing NJ
International Classification:
A61K 31/5513 C07D 487/02
US Classification:
514221000, 540567000
Abstract:
Methods for the racemization of an enantiomer of a 2,3-benzodiazepine molecule into the corresponding racemic mixture under either basic or acidic conditions are described. Furthermore, the invention relates to the conversion of an enantiomer of tofisopam or its metabolites to the corresponding opposite enantiomer.
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