专利检索 ap:("Richter Gedeon Nyrt.") AND inv:"GIZUR, Tibor" 第 1 页

1.

发明授权
BENZENESULPHONAMIDES AND PROCESS FOR THEIR PREPARATION 有权
标题翻译： Benzenesulphonamides及其制备方法

公开(公告)号：EP1539684B1

公开(公告)日：2009-04-15

申请号：EP03793925.3

申请日：2003-09-08

申请人： Richter Gedeon Nyrt.

发明人： GIZUR, Tibor , TÖRLEY, Jozsef , FOGASSY, Elemér , BALINT, Jozsef , EGRI, Gabriella , DEMETER, Adám

IPC分类号： C07C303/40 , C07C311/37 , A61K31/18

CPC分类号： C07C311/37 , A61K31/18 , C07B2200/07 , C07C303/40 , Y02P20/55

摘要： New process for industrial preparation of R-(-)-tamsulosine HCl of formula (I). In this process (R,S)-5-[2-(N-benzyl-amino)-propyl]-2-methoxy-benzenesulphonamide of formula (I), acid addition salts and enantiomers thereof and R-5-[2-[N-(2-ethoxy-phenoxy)-ethyl]-N-benzyl]-amino]-propyl-2-methoxy-benzenesulphonamide of formula (III) are new intermediates. R-(-)-tamsulosine HCl of formula (I) is prepared by reacting the secondary benzylamine of formula (II) with an alkylating agent to R-5-[2-[N-(2-ethoxy-phenoxy)-ethyl]-N-benzyl]-amino]-propyl-2-methoxy-benzenesulphonamide of formula (III), the benzyl protecting group is removed and then HCl salt is formed. The optically active compound of formula (II) is prepared by reductive condensation of (4-methoxy-3-sulphamoyl-phenyl)-acetone and benzylamine and the obtained racemic compound is optically resolved by chiral acid.

2.

发明授权
INDUSTRIAL PROCESS FOR THE SYNTHESIS OF 2-SUBSTITUTED 1-(HYDROXY-ETHYLIDENE)-1,1-BISPHOSPHONIC ACIDS OF HIGH PURITY AND THE SALTS THEREOF 有权
标题翻译： GROSS技术程序用于合成的高纯度的2-取代的1-（羟基亚乙基）-1,1-二膦及其盐的

公开(公告)号：EP1587814B1

公开(公告)日：2009-01-14

申请号：EP04705466.3

申请日：2004-01-27

申请人： Richter Gedeon Nyrt.

发明人： NEU, József , FISCHER, János , FODOR, Tamás , TÖRLEY, József , GIZUR, Tibor , LÉVAI, Sándor , DEMETER, Àdám , PERÉNYI, Éva

IPC分类号： C07F9/58 , C07F9/38

CPC分类号： C07F9/3873 , C07F9/582

摘要： Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof - wherein the meaning of R is 3'-pyridyl or 2'-amino-ethylidene group - from compounds of formula (II) - wherein the meaning of R is as described above - or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.