http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CZ-296521-B6

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filingDate 1998-11-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_15012a8267b5e644c443652546c07297
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publicationDate 2006-04-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CZ-296521-B6
titleOfInvention Method of Preparation 1- [9'H-Carbazol-4'-yloxy] -3 - [{2''- (2'''- &lt; / RTI &gt; methoxy) -phenoxy) -ethyl} -amino] -propan-2-ol (carvedilol)
abstract The present invention relates to a process for the preparation of 1- [9'H-carbazol-4'-yloxy] -3 - [(2 '' - (2 '' - &apos; -methoxy) phenoxy) ethyl} amino] -propan-2-ol , ie carvedilol, as well as its optically active R or S enantiomer, the mixture of the enantiomer and the addition salts of these compounds with an acid, by reacting a 4- (oxiranylmethoxy) -9H-carbazole or its R or S enantiomer with a secondary N- [2- ( The 2 &apos; - &lt; 1 &gt; - methoxy-phenoxy) -ethyl] -benzylamine of formula V is carried out in a protic organic solvent and the 1- [N- {benzyl} -2 &apos; - ({2 ' - &gt; methoxy &lt; / RTI &gt; -ethyl} -amino] -3- [9 '' 'H-carbazol-4' '- yloxy] -propan-2-ol (benzylcarvedilol) is debenzylated by catalytic hydrogenation and the thus obtained 1- [9' H-carbazol-4'-yloxy] -3 - [{2 '' - (2 '' - &quot; methoxy &quot; -phenoxy) -ethyl} -amino] -propan-2-ol, if desired, it is reacted in a manner known per se with inorganic or organic acids to form its acid addition salts, or, if desired, the free baseecarvedilol is released. From its acid addition salts, and if desired, the free base of carvedilol is converted to other acid addition salts and / or enantiomers are separated if desired. Preferably, benzylcarvedilol is not isolated from the reaction mixture in which it was prepared before the debenzylation reaction.
priorityDate 1997-11-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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