New phenylethanolamino- and...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 229/50 (2006.01) C07C 229/34 (2006.01) C07C 229/38 (2006.01) C07C 229/46 (2006.01) C07C 271/18 (2006.01) C07C 271/24 (2006.01) C07D 209/48 (2006.01)

Patent

CA 2061311

IN THE CANADIAN PATENT AND TRADEMARK OFFICE PATENT APPLICATION Entitled: New phenylethanolamino- and phenylethanolaminomethyltetralines, process for the preparation thereof, intermediates in said process and pharmaceutical compositions containing them. in the name of: Domenico BADONE Umberto GUZZI Roberto CECCHI assignee: ELF-SANOFI ABSTRACT OF DISCLOSURE Phenylethanolamino- and phenylethanolaminomethyltetralines of formula (I) Image (I) wherein X represents a hydrogen atom, a halogen atom,a (C1-C4)alkyl group or a trifluoromethyl group, A represents a bond between the -COOR group and the tetraline ring, a (C1-C4)alkylene or a (C2-C4)alkenylene group, R is hydrogen or a (C1-C4)alkyl group, and n is 0 or 1 and their salts, are typically prepared by reaction of an epoxide of formula (IIa) Image (IIa) with a tetraline derivative of formula (III) Image (III) ../.. wherein A and n are as defined above and R' is a (C1-C4)alkyl group, optionally followed by basic hydrolysis to obtain the compounds (I) wherein R is hydrogen. The new compounds show very interesting properties as antidepressant and intestinal spasmolytic agents. The new intermediates of formula (III) are also claimed.

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