1,1,2-triphenyl-but-1-ene derivatives possessing anti-...

Details 1,1,2-triphenyl-but-1-ene derivatives possessing anti-... 1,1,2-triphenyl-but-1-ene derivatives possessing anti-...

C - Chemistry, Metallurgy

07

D

260/602.3

C07D 309/12 (2006.01)

Patent

CA 1220787

ABSTRACT (E)-1-[4'-(2-dialkylaminoethoxy)phenyl]-1-(3'-hydroxyphenyl)- 2-(subst.phenyl)-but-1-enes of the general formula Image in which R in position 3' or 4' represents a methyl group, methoxy group, hydroxy group or a halogen atom and R1 represents a lower alkyl group, and therapeutically acceptable salts thereof, possess a pro- nounced anti-oestrogenic effect and are suited for treatment of hormone- dependent mammary tumors. They can be produced from carbinols of the general formula Image in which R in position 3' or 4' can be a methyl group, methoxy group, acetoxy group or tetrahydropyranyloxy group or a halogen atom, which are dehydrated by the effect of mineral acid with elimination of the protective group, the E-form is isolated from the resulting pair of isomers by crystallisation or by chromotography and optionally it is converted into a therapeutically acceptable salt. - 21 -

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