C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/247.47, 260/
C07D 295/18 (2006.01) C07D 295/185 (2006.01)
Patent
CA 1050023
ABSTRACT OF THE DISCLOSURE The invention relates to a new process for the preparation of benzylamine derivatives of the general formula Image (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 hydroxy- cyclohexyl 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 Image (II) (wherein R1, R4 and Hal are as hereinbefore defined and X represents a nucleophilic leaving group) with a compound of formula Image (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.
194467
Keck Johannes
Kruger Gerd
Dr. Karl Thomae Gesellschaft Mit Chrankter Haftung
Na
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