US 7,521,452 B2
Preparation of pharmaceutical salts of piperazine compounds
Wenxue Wu, Princeton Junction, N.J. (US); Loc Thanh Tran, Parsippany, N.J. (US); Bosco D'Sa, Edison, N.J. (US); Feng Liang, Monmouth Junction, N.J. (US); William Leong, Westfield, N.J. (US); Hong-Chang Lee, Livingston, N.J. (US); Kevin Klopfer, Flemington, N.J. (US); and Vijay Sabesen, Millbrae, Calif. (US)
Assigned to Schering Corporation, Kenilworth, N.J. (US)
Filed on Jan. 05, 2006, as Appl. No. 11/326,155.
Claims priority of provisional application 60/641910, filed on Jan. 06, 2005.
Prior Publication US 2006/0241295 A1, Oct. 26, 2006
Int. Cl. A61K 31/497 (2006.01); C07D 239/02 (2006.01)
U.S. Cl. 514—252.18  [544/335] 9 Claims
 
1. A mixture of rotamers of a salt of a substituted piperazinyl compound of Formula I:

OG Complex Work Unit Drawing
wherein said mixture comprises one rotamer of the salt in a mole percent ratio of greater than 55:45 in comparison with other rotamers present in said mixture, and wherein said salt is prepared by a process comprising reacting said substituted piperazinyl compound with an acid which is benzenesulfonic acid, camphor sulfonic acid, glutaric acid, 2-ketoglutaric acid, nicotinic acid, or benzoic acid in admixture with a solvent which is water, a ketone, an ether, an ester, an alcohol, a nitrile, a hydrocarbon or mixtures thereof.