公开(公告)号：EP0946570B1

公开(公告)日：2002-06-12

申请号：EP97950253.1

申请日：1997-12-15

申请人： Avecia Limited

发明人： BLACKER, Andrew, John ,  FIELDEN, Jan, Michael

IPC分类号： C07F3/06 ,  C07B53/00 ,  C07C29/40

CPC分类号： C07D213/30 ,  C07B53/00 ,  C07B2200/07 ,  C07C29/40 ,  C07F3/06 ,  C07C33/22 ,  C07C33/46 ,  C07C33/20

公开(公告)号：EP1440053A1

公开(公告)日：2004-07-28

申请号：EP02762609.2

申请日：2002-10-02

申请人： Avecia Limited

发明人： ATHERTON, John, Heathcote ,  BLACKER, Andrew, John ,  FIELDEN, Jan, Michael ,  JACKSON, David, Anthony ,  DODMAN, David

IPC分类号： C07C251/86 ,  C07C251/82 ,  C07C251/74 ,  C07C249/16 ,  C07C241/02 ,  C07C243/22 ,  C07C243/20 ,  C07C243/12

CPC分类号： C07C249/16 ,  C07C251/86

摘要： A process for the preparation of a compound of formula (I): wherein Ar represents an optionally substituted aromatic carbocycle or heterocycle, and R?1 and R2¿ independently represent hydrogen, C¿1-10?alkyl, C(O)C1-10alkyl or optionally substituted aryl provided that R?1 and R2¿ are not both hydrogen which process comprises reacting together a compound of formula (II): Ar-X, wherein Ar is as defined in relation to formula (I) and X represents a leaving group with a compound of formula (III): wherein R?1 and R2¿ are as defined in relation to formula (I) under aqueous conditions in the presence of a Pd (II) salt, a ligand and a Group I or Group II metal hydroxide base at a pH greater than 7. Compounds of formula (I) may be hydrolysed to the corresponding hydrazine.