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Cytotoxic ester derivatives of the mammary-tumor-inhibiting antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane

Schwarz, Walter ; Hartmann, Rolf W. ; Engel, Juergen ; Schneider, Martin R. ; Schönenberger, Helmut


The synthesis of the bisacrylate I (R = CH2:CHCO2) (II), the bis-beta -chloropropionate I (R = ClCH2CH2CO2) (III) and the bis-beta -bromopropionate I (R = BrCH2CH2CO2) (IV) of the partial antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane I (R = OH) (V) by condensation V with corresponding acid chloride is described. In the case of III and IV the introduction of the beta -haloester ...


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