PROCESS FOR THE PREPARATION OF BENZYLAMINES

摘要

The invention relates to a new process for the preparation of benzylamine derivatives of the general formula (I)(wherein Hal represents a chlorine or bromine atom; R1 represents a hydrogen, chlorine or bromine atom; R2 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms; and either R3 represents a cyclohexyl or hydroxycyclohexyl group and R4 represents a hydrogen atom or R3 represents an isopropylaminocarbonylmethyl or a morpholine-carbonylmethyl group and R4 represents a hydrogen atom or a benzyl group) and acid addition salts thereof, which process comprises reacting a compound of formula (II) (wherein R1, R4 and Hal are as hereinbefore defined and X represents a nucleophilic leaving group) with a compound of formula (III)(wherein R2 and R3 are as hereinbefore defined) and if desired subsequently converting the compound of formula I thereby obtained into an acid addition salt thereof having valuable physiological properties, in particular a secretolytic, antitussive and/or respiration stimulating activity. The new process comprises aminating a reactive derivative of the corresponding benzyl alcohol. Examples of the preparation of some benzylamine derivatives by means of the new process are given.