Process for the production of basic triphenylalkene derivatives

Details Process for the production of basic triphenylalkene derivatives Process for the production of basic triphenylalkene derivatives

C - Chemistry, Metallurgy

07

D

260/603.2, 260/2

C07D 295/08 (2006.01) C07D 295/092 (2006.01)

Patent

CA 1072093

ABSTRACT OF THE DISCLOSURE This invention relates to a process for preparing triphenylalkene derivatives of the general formula I Image (I) wherein R1 and R2 may denote identical or different C1-4 alkyl groups or together with the adjacent nitrogen atom they may denote a nitrogenous heterocyclic group containing also another heteroatom, whereas R3 denotes a C1-4 alkyl group, and their salts and /Z/ and /E/ isomers, characterized in that the /Z/ or /E/ isomer or the mixture of these isomers of an aryl halide of the general formula II Image (II) wherein R3 has the above-given meaning and X denotes a halogen atom, is reacted with an aminoethanol derivative of the general formula III R1R2N - CH2 - CH2 - OM (III) wherein R1 and R2 have the same meaning as above and M denotes hydrogen or an alkali metal, preferably a sodium or potassium atom. The products of the process are known to posses an antiestrogen effect; one of them: the /Z/- 1,2-diphenyl-1- {p-[2-(dimethylamino) - ethoxy]-phenyl} - 1-bitene has been applied also therapeutically for the treatment of hormone-dependent mammil- lary cancer.

271083

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