Process for preparing 1-[9?H-carbazol-4?-yloxy]-3-[{2??-(2???-phenoxy)ethyl}amino]propan-2-ol [carvedilol]

Zpusob prípravy karvedilolu vzorce I jakoz i jehoadicních solí s kyselinou, spocívající v tom, ze sekundární amin N-[2-(2'-<methoxy>fenoxy)ethyl]benzylamin vzorce V se nechá reagovat s epichlorhydrinem známým zpusobem, nacez takto vzniklá chlor sloucenina 1-[N-{benzyl}-2'-({2''-<methoxy>fenoxy)ethyl}amino]-3-[chlor]propan-2-ol vzorce VI se nechá reagovat s 4-(hydroxy)-9H-karbazolem vzorce VII, nacez se takto vzniklý benzylkarvedilol vzorce VIII debenzyluje katalytickou hydrogenací provedenou známým zpusobem, a pokud je treba, pak takto pripravený 1-[9'H-karbazol-4'-yloxy]-3-[{2''-2'''-fenoxy)ethyl}amino]propan-2-ol se nechá reagovat sanorganickými nebo organickými kyselinami, címz se získá adicní sul s kyselinou, nebo pokud je treba, tak se uvolní báze karvedilolu vzorce I ze svých adicních solí s kyselinou, a pokud je treba, takse volná báze karvedilolu konvertuje na dalsí adicní soli s kyselinou a/nebo, pokud je treba, tak se provede separace enantiomeru. In the present invention, there is disclosed a process for preparing carvedilol of the general formula I as well as acid addition salts thereof wherein the preparation process is characterized by reacting secondary amine, i.e. N-[2-(2'-phenoxy)ethyl]benzylamine of the general formula V with epichlorohydrin whereupon so formed chloro compound i.e. 1-[N-{benzyl}-2'-({2''-phenoxy)ethyl}amino]-3-[chloro]propan-2-ol of the general formula VI is brought into reaction with 4-(hydroxy)-9H-carbazole of the general formula VII. Subsequently so formed benzyl carvedilol of the general formula VIII is subjected to removal of benzyl by catalytic hydrogenation being carried out by a known method and when need may be so prepared 1-[9'H-carbazol-4'-yloxy]-3-[{2''-2'''-phenoxy)ethyl}amino]propan-2-ol is brought into reaction with inorganic or organic acids to thereby obtain an acid addition salt, when need may be a carvedilol base of the general formula I is released from its acid addition salts and if need may be a free carvedilol base can be converted to another acid addition salt and if need may be separation of enantiomers can be carried out.