MENDES, ZITA,BAPTISTA, JOANA,MARTIN, DIONISIO,HEGGIE, WILLIAM
申请号：
CA2593010
公开号：
CA2593010C
申请日:
2005.01.18
申请国别(地区):
CA
年份:
2012
代理人:
摘要：
A process for producing tamsulosin of formula (I) and pharmaceuticallyacceptable addition salts, thereof comprises the steps of : a) Reactingcompound R,R-[2-(4-methoxy-phenyl)-1-methyl-ethyl]-(1-phenyl-ethyl)-amine offormula (II) or a salt thereof (II) with chlorosulfonic acid with or withoutan organic solvent, to obtain compound R,R-2methoxy-5-[2-(1-phenyl-ethylamino)-propyl]-benzenesulfonic acid of formula (III) b) Hydrogenolysis of compoundR,R-2-methoxy-5-[2-(1-phenyl-ethylamino)-propyl]- benzenesulfonic acid offormula III or a salt thereof carried out in an alcohol in the presence of apalladium catalyst using hydrogen or a source of hydrogen, to obtain compoundR-(-)-5-(2-amino-propyl)-2-methoxy-benzenesulfonic acid of formula (IV)c)Reacting primary amine R-(-)-5-(2-amino-propyl)-2-methoxy-benzenesulfonicacid of formula (IV), or a salt thereof, with a compound of formula (V)wherein X represents an halogen atom selected from the group consisting ofC1；Br and I, to obtain 5- [(2R)-2-[2-(2-ethoxy-phenoxy)-ethylamino]-propyl]-2-methoxy-benzenesulfonic acid compound of formula (VI) d) Reacting compound offormula (VI) with an halogenating agent, to obtain the correspondingsulfonylchloride of formula (VII). e)Reacting compound VII with ammonia toobtain compound I.
