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

摘要

The subject matter of the invention is a process for preparing 1-Ä9'H-carbazol-4'-yloxyÜ-3-Ää2''-(2'''-<methoxy>--phenoxy)-ethylü-aminoÜ-propan-2-ol as well as acid addition salts of this compound, in which the H-Ä2-(2'-<methoxy>--phenoxy)-ethylÜ-benzylamine is reacted with epichlorohydrin, the thus formed 1-ÄN-äbenzylü-2'-(ä2''-<methoxy>-phenoxy)--ethylü-aminoÜ-3-ÄchloroÜ-propan-2-ol is reacted with 4-(hydroxy)-9H-carbazole and the thus formed 1-ÄN-äbenzylü-- 2'-(ä2''-<methoxy>-phenoxy)- ethylü-aminoÜ-3-Ä9'''H-carbazol-- 4'''-yloxyÜ-propan-2-ol is debenzylated by catalytic hydrogenation and, if desired, the 1-Ä9'H-carbazol-4'-yloxyÜ--3-Ää2''-(2'''-<methoxy>-phenoxy)-ethylü-aminoÜ-propan-2-ol thus obtained is reacted with acids to yield acid addition salts thereof or, if desired, liberating the free 1-Ä9'H--carbazol-4'-yloxyÜ-3-Ää2''-(2'''-<methoxy>-phenoxy)-ethylü--aminoÜ-propan-2-ol base from acid addition salts thereof and, if desired, converting the free 1-Ä9'H-carbazol-4'--yloxyÜ-3-Ää2''-(2'''-<methoxy>-phenoxy)-ethylü-aminoÜ--propan-2-ol base into other acid addition salts and/or, if desired, separating the enantiomers.