ES433897A1 - Procedure for the preparation of new bencilamines. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure for the preparation of new benzylamines of the general formula I **(See formula)** wherein R1 signifies a hydrogen atom or an optionally substituted aliphatic or aromatic acyl radical; R2 signifies a hydrogen, chlorine or bromine atom; R3 signifies a fluorine atom, a straight or branched chain C 1 -C 4 alcohol radical, a trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, 1-hydroxyethyl group as well as the amino-methyl group of the formula **(See formula)** wherein R6 and R7, which may be the same or different, represent alcohol, cycloalcohyl or hydroxy-chloalcohyl groups or together with the nitrogen atom a pyrrolidine, piperidine or morpholine ring, R4 and R5, which may be the same or different, represent hydrogen atoms, alcohol radicals with 1 to 5 straight or branched chain carbon atoms, which may be substituted with one or two hydroxy groups, alkenyl radicals with 2 to 4 carbon atoms, cycloalcohyl radicals with 5 to 7 carbon atoms, optionally substituted with one or two hydroxy groups, benzyl groups, marpholinocarbonylmethyl or together with the nitrogen atom signify a pyrrolidine, piperidine, hexamethylenamine, morpholine, N-methyl-piperazine or camfidine ring, as well as their physiologically compatible acid addition salts thereof. organic or inorganic acids, characterized in that an aldehyde of the general formula II is reacted, **(See formula)** wherein R1, R2 and R3 are as initially defined, with an amine of general formula III, **(See formula)** wherein R4 and R5 are as initially defined, or with the corresponding formamide in the presence of formic acid; and, if desired, a compound of the general formula I obtained in which R3 represents a cyano group, is transformed by partial hydrolysis into the corresponding carbamoyl compound of the general formula I, and/or a compound obtained of the general formula I, in which R1 represents a hydrogen atom and R2, R3, R4 and R5, with the exception of the radicals containing a hydrogen atom capable of reacting, are as initially defined, is acylated if desired later, and/or a compound obtained from the general formula I is transformed, if desired, into its physiologically compatible salts with organic or inorganic acids. (Machine-translation by Google Translate, not legally binding)