Neue Aminoalkohole und Verfahren zur Herstellung derselben

摘要

1,199,330. Aminoalcohols. RICHTER GEDEON VEGYESZETI GYAR RT. 12 Sept., 1967 [24 Sept., 1966], No. 41645/67. Heading C2C. Racemic and optically active compounds of the general Formula (I): (R 1 = H, halogen, C 1-5 alkyl or alkoxy; R 2 =H, C 1-5 alkyl; R 3 =H, branched alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl; R 4 = cycloalkyl, alkenyl or (when R 3 is not H) branched alkyl; or NR 3 R 4 = heterocyclic ring provided that when the ring contains a further heteroatom it is not N) and their acid addition salts, are prepared by (a) reacting a compound of the Formula (II): (X=halogen) and/or a compound of the Formula (III): with R 3 R 4 NH and reducing the resulting nitrophenylalkanolamine, (b) hydrolysing or alcoholysing a compound of the Formula (IV): (R 5 = alkanoyl, aroyl, alkylsulphonyl, arylsulphonyl), (c) hydrogenolysing a compound of the Formula (IV) but in which R 5 = alkylsulphonyl, arylsulphonyl, benzyl, or (d) reducing a compound of the formula in one or two steps, optionally followed by salt formation. If an optically active product is required an optically active starting material may be used or resolution effected at any desired stage. The above compounds are antidepressants and hypotensive agents, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.