ChemInform Abstract: Synthesis and Biological Evaluation of a Series of 1,1-Dichloro-2,2,3- triarylcyclopropanes as Pure Antiestrogens.
Abstract
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ChemInform Abstract
Reaction of the deoxybenzoins (I) with the 4-alkoxyphenylmagnesium bromides (II) followed by dehydration yields the triarylethylenes (III) as a mixture of E/Z-isomers. Addition of dichlorocarbene forms the dichlorocyclopropyl derivatives (V) and (VI). The latter are dealkylated and then coupled with (2-chloroethyl)dimethylamine hydrochloride (VIII) to give the corresponding O-alkylation products ( IX). Further reactions are described in the original paper. None of the tested compounds show estrogenic activity, but (IXa) and (IXb) exhibit dose-dependent antiuterotropic effects in vivo.
