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专利名称：PROCESS FOR THE PREPARATION OF
CARVEDILOL
发明人：KANKAN, Rajendra Narayanrao,RAO,
Dharmaraj Ramachandra, 4/403 GardenEnclave
申请号：EP05744187.5申请日：20050519公开号：EP1756057B1公开日：20100804
摘要：A process for the preparation of carvedilol of formula (I) (I) either inenantiomeric substantially pure form, or as an enantiomeric mixture, optionally as apharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol offormula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol offormula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture,and if desired reacting the thus formed carvedilol of formula (I) with an inorganic ororganic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired,separating the enantiomers. The above process is characterised in that reaction of said2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium. The presentinvention further provides carvedilol of formula (I) prepared by a process as describedabove, and pharmaceutical compositions containing the same and therapeutic uses
thereof.
申请人：CIPLA LTD
地址：IN
国籍：IN
代理机构：Curtis, Philip Anthony
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