公开(公告)号：EP1711466A1

公开(公告)日：2006-10-18

申请号：EP05713069.2

申请日：2005-02-07

申请人： Teva Pharmaceutical Industries Ltd

发明人： DOLITZKY, Ben-Zion ,  HILDESHEIM, Jean ,  BERLIN, Alisa ,  EISEN-NEVO, Hagit ,  LERMAN, Ori

IPC分类号： C07D215/22

CPC分类号： C07D215/227

摘要： The invention encompasses the synthesis of aripiprazole from BBQ and DCP, and comprises mixing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril (BBQ) and 1-(2,3­-dichlorophenyl)piperazine hydrochloride (DCP) in the presence of at least one base and at least one organic solvent to form a reaction mixture; heating the reaction mixture for a sufficient amount of time to effect the reaction; and isolating aripiprazole. The invention also encompasses the use of phase transfer catalysts in synthesizing aripiprazole from BBQ and DCP.

公开(公告)号：EP1812428A2

公开(公告)日：2007-08-01

申请号：EP05852062.8

申请日：2005-11-21

申请人： Teva Pharmaceutical Industries Ltd

发明人： IZSAK, Reuven ,  LERMAN, Ori ,  KOLTAI, Tamas ,  ARONHIME, Judith ,  PINCHASOV, Michael ,  EISEN-NEVO, Hagit

IPC分类号： C07D413/04 ,  A61K31/422 ,  A61P25/06

CPC分类号： C07D413/06

摘要： The invention encompasses novel crystalline forms of zolmitriptan herein defined as Form B, D, C, E, F, G, H, I, J, K, M, N, O, P, Q, R, S, or Amorphous and to methods of making thereof. The invention also encompasses methods of making zolmitriptan crystalline Form A.