METHOD OF PRODUCING 1,1,2-TRIPHENYLPROPENE DERIVATIVES OR STEREOISOMERS,OR STEREOISOMER MIXTURE,OR ACID-ADDITIVE SALTS THEREOF

摘要

New 1,1,2-triphenylpropane and -propene derivatives of the general formula (I), wherein A and B each stand for hydrogen or they form together a valence bond, X and Y are identical or different and stand for phenyl group or a phenyl group having a halogen, hydroxy methoxymethoxy, C1-6 alkoxy or benzyloxy substituent in the para position, R1 is a C1-6 alkyl, epoxyalkyl, azidoalkyl, methoxymethyl or benzyl group or a group of the general formula (II), wherein R2 and R3 each represent hydrogen or a C1-6 alkyl, hydroxyalkyl or haloalkyl group, or R2 and R3 form together with the adjacent nitrogen atom an up to 8-membered heterocyclic group, an up to 6-membered heterocyclic group optionally containing further hetero atom(s), which heterocyclic groups optionally have a lower alkyl or hydroxyalkyl substituent, a guanidino group, an aminoguanidino group or a nitroguanidino group, with the proviso that if A and B form together a valence bond and X and Y each stand for phenyl or X is phenyl and Y is p-methoxyphenyl, R1 may not stand for a dimethylaminoethyl, diethylaminoethyl, pyrrolidinoethyl, a piperidinoethyl or morpholinoethyl group in the (Z) isomers, stereoisomers and isomeric mixtures thereof, and acid addition salts of the basic compounds of the general formula (I) exert oestrogenic or antioestrogenic effects and furthermore inhibit the growth of the mammary tumor induced by 7,12-dimethyl-benz(a)anthracene.