US 7,541,355 B2
Conversion process for 2,3-benzodiazepine enantiomers
Yong Victoria Wei, Branchburg, N.J. (US); Naidaong Ye, Malvern, Pa. (US); Kimm Galbraith, Spring City, Md. (US); Jianfeng Shi, Baltimore, Md. (US); Wuyi Wang, Silver Spring, Md. (US); Yungen Xu, Baltimore, Md. (US); and Mallikarjun Reddy Ravi, Baltimore, Md. (US)
Assigned to Vela Acquisition Corporation, Iselin, N.J. (US)
Filed on May 23, 2005, as Appl. No. 11/135,100.
Prior Publication US 2006/0264421 A1, Nov. 23, 2006
Int. Cl. A61P 25/22 (2006.01); A61K 31/551 (2006.01); C07D 243/02 (2006.01)
U.S. Cl. 514—221  [540/567] 18 Claims
 
1. A method for racemizing an enantiomer of tofisopam to its racemate, the method comprising (a) reacting the enantiomer with one or greater base equivalent of an organic base at a temperature below 20° C. and (b) quenching the reaction with a proton source, thereby obtaining the racemate from the enantiomer.