| 摘要 |
The present invention relates to stereoselective synthesis of 7-±-substituted estra-4-ene-3,17-diones. Such compounds are valuable intermediates in the synthesis of 7-±-substituted estra-1,3,5(10)-triene-3,17-diols. Key step in this synthesis is reacting a 3-keto-4,6-estradiene with a Grignard reagent selected from the group consisting of a magnesium-halide alkyl halide having at least 3 carbon atoms, a magnesium-halide alkenyl halide having at least 3 carbon atoms, and a magnesium-halide alkynyl halide having at least 3 carbon atoms, in the presence of a catalyst system comprising CuI. The obtained 7±-alkyl, alkenyl and alkynyl halides can be used for the synthesis of pharmaceutically actice 7-±-substituted estra-1,3,5(10)-triene-3,17-diols (antiestrogens).
|
