ES433896A1 - 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 branched-chain or branched-chain 1 to 4-carbon alcohol radical, a trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl group, 1-hydroxyethyl as well as the aminomethyl group of the formula **(See formula)** wherein R6 and R7, which may be the same or different, represent alcohol, cycloalcohyl or hydroxycycloalcohyl groups or together with the nitrogen atom a pyrrolidine, piperidine or morpholine ring; R4 represents a hydrogen atom, an alcohol radical with 1 to 5 straight or branched chain carbon atoms, which may be substituted with one or two hydroxy groups, an alkenyl radical with 2 to 4 carbon atoms, a cycloalkoxy radical with 5 to 7 carbon atoms optionally substituted with one or two hydroxy groups, a benzyl or morpholinocarbonylmethyl group; and R5 signifies a straight or branched chain alcohol radical with 1 to 5 carbon atoms, a cycloalcohyl radical with 5 to 7 carbon atoms, a benzyl or morpholinocarbonylmethyl group, as well as its acid addition salts physiologically compatible with organic acids or inorganic, characterized in that it undergoes alcoholization of a compound of the general formula **(See formula)** wherein R1, R2, R3 and R4 are as initially defined, with a compound of the general formula III R5 - W (III) where R5 has the initially mentioned meanings, and W represents a halogen atom or a sulfonic acid radical; 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)