Process for the preparation of substituted 3-aryl-butyl-amine compounds

摘要

Disclosed is a process for the preparation of a substituted 3-aryl-butyl-amine compound of the general formula I wherein R7 and R8 in each case independently of one another are chosen from H or C1-3-alkyl, branched or unbranched, saturated or unsaturated, unsubstituted or mono- or polysubstituted, and wherein the rest of the substituents are disclosed within the specification, in each case in the form of a pure stereoisomer, racemate or in the form of a mixture of stereoisomers in any desired mixing ratio, or in each case in the form of a physiologically acceptable salt, or in each case in the form of a solvate, in which a first step a) a 1-amino-3-aryl-butan-3-ol compound of the general formula II wherein the substituents are defined within the specification and in each case optionally in the form of a pure stereoisomer, racemate or in the form of a mixture of stereoisomers in any desired mixing ratio, or in each case in the form of a physiologically acceptable salt, or in each case in the form of a solvate, is employed and elimination is carried out under the action of an acid to give a substituted 3-aryl-but-3-enyl-amine compound of the general formula III wherein the substituents are disclosed in the specification, in each case optionally in the form of a pure stereoisomer, racemate or in the form of a mixture of stereoisomers in any desired mixing ratio, or in each case in the form of a physiologically acceptable salt, or in each case in the form of a solvate, and in a second step b) the substituted 3-aryl-but-3-enyl-amine compound according to the general formula III formed is then hydrogenated under the participation of a metal catalyst and hydrogen to give a substituted 3-aryl-butyl-amine compound of the general formula I.