发明名称 |
BENZENESULPHONAMIDES AND PROCESS FOR THEIR PREPARATION |
摘要 |
<p>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]-Nbenzyl]-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.</p> |
申请公布号 |
EP1539684(A1) |
申请公布日期 |
2005.06.15 |
申请号 |
EP20030793925 |
申请日期 |
2003.09.08 |
申请人 |
RICHTER GEDEON VEGYESZETI GYAR R.T. |
发明人 |
GIZUR, TIBOR;TOERLEY, JOZSEF;FOGASSY, ELEMER;BALINT, JOZSEF;EGRI, GABRIELLA;DEMETER, ADAM |
分类号 |
C07C303/40;C07C311/37;(IPC1-7):C07C303/40;A61K31/18 |
主分类号 |
C07C303/40 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|