公开(公告)号：EP2332916A3

公开(公告)日：2011-08-03

申请号：EP10156733.7

申请日：2010-03-17

申请人： Krka Tovarna Zdravil, D.D., Novo Mesto

发明人： Zupet, Rok ,  Pecavar, Anica ,  Iskra, Jernej ,  Ruzic, Milos ,  Kolenc, Ivanka

IPC分类号： C07D215/58

CPC分类号： C07D215/58

摘要： The present invention describes a novel process for the preparation of marbofloxacin and intermediate thereof comprising reaction of ammonium hydroxide of formula III, NR 1 R 2 R 3 R 4 wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group of H, alkyl, alkylaryl, aryl and/or heteroaryl, with compound of formula II,

wherein R is selected from H, alkyl, arylalkyl, alkali metal cation, , NH 4 cation, NR 1 R 2 R 3 R 4 cation; X is halogen, such as chloro, bromo, fluoro, piperazinyl, which may be substituted or unsubstituted, and R' is selected from H, formyl or COOAlkyl.

公开(公告)号：EP2332916A2

公开(公告)日：2011-06-15

申请号：EP10156733.7

申请日：2010-03-17

申请人： Krka Tovarna Zdravil, D.D., Novo Mesto

发明人： Zupet, Rok ,  Pecavar, Anica ,  Iskra, Jernej ,  Ruzic, Milos ,  Kolenc, Ivanka

IPC分类号： C07D215/58

CPC分类号： C07D215/58

摘要： The present invention describes a novel process for the preparation of marbofloxacin and intermediate thereof comprising reaction of ammonium hydroxide of formula III, NR 1 R 2 R 3 R 4 wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group of H, alkyl, alkylaryl, aryl and/or heteroaryl, with compound of formula II,

wherein R is selected from H, alkyl, arylalkyl, alkali metal cation, , NH 4 cation, NR 1 R 2 R 3 R 4 cation; X is halogen, such as chloro, bromo, fluoro, piperazinyl, which may be substituted or unsubstituted, and R' is selected from H, formyl or COOAlkyl.

摘要翻译： 本发明描述了制备马氟沙星及其中间体的新方法，其包括式III的氢氧化铵，NR 1 R 2 R 3 R 4的反应，其中R 1，R 2，R 3和R 4独立地选自 H，烷基，烷基芳基，芳基和/或杂芳基与式II化合物反应，其中R选自H，烷基，芳烷基，碱金属阳离子，NH 4阳离子，NR 1 R 2 R 3 R 4阳离子; X是卤素，例如氯，溴，氟，哌嗪基，其可以是取代或未取代的，R'选自H，甲酰基或COOA烷基。